Apoptose

Compound C11 inhibits 14-3-3η protein (KD: 35 μM), targets liver cancer cells, blocks G1-S phase, and induces apoptosis.

Etalocib (LY293111) sodium is an orally active leukotriene B4 (LTB4) receptor antagonist with a Ki value of 25 nM for inhibiting [3H]LTB4 binding. It exhibits an IC50 of 20 nM against LTB4-induced calcium mobilization. Additionally, Etalocib sodium can induce apoptosis.

Ferroptosis-IN-15 (compound 12) serves as an effective inhibitor of ferroptosis, exhibiting EC50 values of 0.76 μM and 0.67 μM in A375 cells and 786-O cells, respectively. It acts as a potential iron chelator and radical-scavenging antioxidant.

Soquelitinib (CPI-818) is a selective ITK inhibitor， inhibits tumor growth,T-cell, up-regulatCXCR3, IFNγ, TNFα, and CD107a expression in normal CD8 cells.

Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.

P53 Activator 11 (compound A-1) is a highly effective p53 activator, demonstrating an EC50 value of 0.478 µM for p53 (Y220C). It holds potential for cancer research [1].

N-Nitrosonornicotine, a tobacco-specific nitrosamine, exhibits carcinogenic and mutagenic properties, and is capable of inducing micronuclei in C3A cells. Additionally, N-Nitrosonornicotine can form DNA adducts.

PD-L1/Nampt-IN-1 is an orally active inhibitor that targets both PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase), with IC50 values of 63 nM and 582 nM, respectively. It exhibits cross-species affinity, with KD values of 52.6 nM for hPD-L1 and 49.1 nM for mPD-L1. This compound effectively suppresses tumor growth by activating the tumor immune microenvironment and is applicable in melanoma research.

Apoptosis inducer42 is an apoptosis inducer that triggers late-stage apoptosis and inhibits the secretion of IL-6. It exhibits high cytotoxicity toward cancer cells and is applicable in cancer research, including studies on colon cancer.

Tuspetinib (HM43239) dihydrochloride is a selective FLT3 inhibitor with oral bioactivity, exhibiting IC50 values of 1.1 nM for FLT3 wild type, 1.8 nM for FLT3ITD mutant type, and 1.0 nM for FLT3D835Y mutant type. As a reversible type I inhibitor, it directly suppresses FLT3 kinase activity and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride inhibits the proliferation of leukemia cells and induces apoptosis (apoptosis).

Neuroprotective agent 11 (Compound 1a) is an orally active polyphenolic compound that offers significant protection against cerebral ischemia. Its primary activities include inhibiting neuronal inflammation and apoptosis, reducing cerebral infarct size, and improving behavioral symptoms in mice with cerebral ischemia. The mechanism involves downregulating inflammatory factors (iNOS, COX-2) and apoptotic proteins (cleaved-Caspase3, p53). Neuroprotective agent 11 is applicable for research in ischemia-related brain diseases, such as ischemic stroke.

Vitamin K5 (hydrochloride), a naphthoquinone compound, exhibits trichomonacidal activity in vitro and can be utilized for anti-infection research [1].

(±)-Perillaldehyde exhibits antidepressant effects in mice with stress-induced depressive-like behavior by modulating the olfactory nervous system. Additionally, it demonstrates anti-inflammatory activity by activating JNK in RAW264.7 cells and suppressing the expression of TNF-α, with an IC50 value of 171.7 μM.

BRD-K56819078, a Bcl-2 inhibitor, significantly reduces the burden of senescent cells and the mRNA expression of aging-related genes in the kidneys. It exerts its anti-aging effects by inhibiting cell apoptosis (apoptosis).

Anticancer agent 183 (compound 4h) exhibits potent inhibition of matrix metalloproteinase-9 (MMP-9), reducing its viability by more than 75% at a concentration of 100 μg/mL. Additionally, it demonstrates significant anticancer activity, with an IC50 value of <0.14 μM against the A549 cell line and induces apoptotic [1] processes.

NLRP3-IN-81 (N102) is an inhibitor capable of crossing the blood-brain barrier, effectively countering NLRP3 inflammasome-dependent pyroptosis with an EC50 of 0.029 μM for Nigericin-induced pyroptosis. It significantly suppresses caspase-1 activation and IL-1β release that depend on NLRP3. Additionally, NLRP3-IN-81 disrupts the interaction between NLRP3 and the adaptor protein ASC, while inhibiting ASC oligomerization. This compound is applicable in research on pyroptosis-related diseases, such as inflammatory bowel disease and type 2 diabetes.

Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.

Citric acid-13C2 is a 13C-labeled form of citric acid. Citric acid serves as a preservative and food additive. It induces apoptosis in HaCaT cells and causes cell cycle arrest at the G2/M and S phases. Additionally, citric acid contributes to liver oxidative damage by reducing antioxidant enzyme activity. It also functions as an acidulant, emulsifier, chelating agent, and buffer, with extensive applications across multiple industries.

eIF4A-IN-1 is an eIF4A inhibitor used in tumor research.

TMC353121 is an effective inhibitor of respiratory syncytial virus fusion (pEC50: 9.9).

eIF4A-IN-3 (Compound 71E) is an inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound can be utilized as a cytotoxic payload for antibody-drug conjugates (ADCs).

Antitumor agent-51 targets osteosarcoma with 21.9 nM IC50, high selectivity, and low toxicity.

YW3-56: PAD2 & PAD4 inhibitor (IC50 = 0.5-5 μM), halts U2OS cell growth (IC50 ~2.5 μM), reduces S-180 & MDA-MB-231 tumor growth in mice.

HI042 is an FMS-like tyrosine kinase 3 (FLT3) inhibitor, showing an IC50 value of 0.62 μM for MOLM-13 cells, 0.33 μM for MV4-11 cells, and 0.89 μM for OCI-AML3 cells. It selectively reduces the survival rate of FLT3-internal tandem duplication (FLT3-ITD) positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes colony-forming ability. HI042 is applicable for acute myeloid leukemia (AML) research.

3′-Hydroxyflavanone is a cyclized flavonoid with anti-tumor properties that induces apoptosis in HeLa cells.

Rafutrombopag is a thrombopoietin (TPO) agonist.

PKM2-IN-6 (compound 7d) is an orally active PKM2 inhibitor (IC50=23 nM) capable of inducing apoptosis and G2 cell cycle arrest. It reduces PKM1 and PKM2 expression at the mRNA level, exhibits antitumour activity, and is suitable for investigating triple-negative breast cancer (TNBC).

<p>EGFR-IN-134 (compound 3f) is a triazolo[3,4-a]quinoline derivative and functions as a potent EGFR inhibitor with an IC50 of 0.023 µM. It induces apoptosis and necrosis in cells, and causes cell cycle arrest in the G2/M and pre-G1 phases. EGFR-IN-134 modulates the expression of apoptosis-regulating proteins by downregulating anti-apoptotic protein Bcl2 and upregulating pro-apoptotic proteins p53, Bax, and caspases 3, 8, and 9, demonstrating significant antiproliferative and anticancer activities.</p>

p53 Activator 8 (compound 5), a potent p53 activator, exhibits significant anti-proliferative effects on MCF7 breast cancer cell lines, demonstrating an IC 50 value of 0.5 μM [1] [2].

RET-IN-30 (Compound 28) is a RET inhibitor that exhibits inhibitory activity against both wild-type RET and some of its mutants. It is capable of inhibiting the proliferation of A549 cells and demonstrates antitumor properties.

ADAR1-IN-1 is a potent ADAR1 inhibitor. It significantly suppresses the proliferation of DU-145 cells (IC50 = 1.11 μM), inhibits colony formation, migration, and invasion, and induces cell cycle arrest and apoptosis. ADAR1-IN-1 effectively and safely impedes tumor growth and can be utilized in prostate cancer (PCa) research.

FHND5071 (1H) is a selective inhibitor of RET (rearranged during transfection) tyrosine kinase. It shows potential for research applications in RET-driven cancers, such as thyroid and lung cancer.

SJ11646 is a Dasatinib-based LCK PROTAC degrader with a DC50 of 0.00838 pM. It exhibits potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, significantly prolongs LCK signal inhibition, and induces apoptosis in T-ALL cells. SJ11646 binds with high affinity to 51 human kinases, particularly ABL1, KIT, and DDR1. In mouse models of T-ALL, SJ11646 demonstrates exceptional anti-leukemic efficacy.

<p>NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.</p>

<p>ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.</p>

MG-B-28, a BTLA-HVEM inhibitor, demonstrates an IC50 value of 906 nM. It promotes T cell activation dose-dependently by inhibiting the interaction between BTLA and HVEM.

Compound 510B, also known as p53 Activator 12, is a powerful activator of p53. This compound specifically interacts with mutant p53 to restore its DNA-binding function.

VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.

T-1-PMPA, a potent EGFR inhibitor, demonstrates apoptotic properties and effectively inhibits EGFR WT and EGFR 790m, with IC50 values of 86 nM and 561.73 nM, respectively [1].

MLS-0053105, a chloromaleimide, functions as a selective inhibitor of BFL-1, exhibiting an IC50 of 0.4 µM against Bfl-1/F-Bid. Its inhibitory potency is over tenfold lower for Bcl-W, Bcl-2, and Bcl-XL, and it shows no activity against Bcl-B and Mcl-1.

ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2 that promotes the accumulation of DSBs and the degradation of ERK1/2 expression. This compound decreases BCL-2 levels and induces DNA damage by inhibiting PARP and ERK1/2. Additionally, ERK1/2 inhibitor 11 activates caspase 3 to induce apoptosis.

Ferrostatin-1 diyne (Fer-1 diyne) (compound 2) serves as an inhibitor of ferroptosis, accumulating in cellular lysosomes, mitochondria, and the endoplasmic reticulum. It notably inhibits ferroptosis independently of lysosomal and mitochondrial activity.

NDs-IN-1 (Compound 3g) is a novel non-covalent multi-target inhibitor that inhibits the activities of key enzymes such as hBACE-1, hAChE, and hMAO-B, and is primarily used in the study of neurodegenerative diseases [1].

WEHI-9625 is a tricyclic sulfone small molecule apoptosis inhibitor (EC50: 69 nM).

RIPK3-IN-6 (compound 1) is a type I RIPK3 inhibitor with low selectivity within the RIPK family, particularly in relation to RIPK2 activity.

DeFer-2 is a ferritin PROTAC degrader (Kd= 17.1 μM). It triggers the degradation of ferritin leading to the accumulation of free iron ions and an increase in ROS, which subsequently initiates caspase 3-GSDME mediated pyroptosis in cancer cells. DeFer-2 significantly inhibits tumor growth and extends the survival of mice with subcutaneous B16F10 tumors, and it is useful for melanoma research.

SMIP34 is an inhibitor of PELP1, binding to this target with a dissociation constant (Kd) of 37.4 μM. It demonstrates efficacy in inhibiting the proliferation of cancer cells and tumor progression. Specifically, SMIP34 is effective in breast cancer research, showing activity against wild-type (WT), mutant (MT) estrogen receptor-positive (ER+), and treatment-resistant (TR)-ER+ breast cancers.

Pamiparib (BGB-290) is a selective PARP inhibitor that blocks DNA repair and promotes apoptosis.

<p>eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.</p>

Autophagy-IN-1 blocks autophagy in cancer cells, hinders tumor growth in mice, and aids in studying colorectal cancer.

<p>BRD-K44839765 selectively targets Bcl-2, exhibiting an IC50 of 5.6 μM in IMR-90 cells. This compound is also orally active.</p>

BRD-K20733377 is a Bcl-2 inhibitor that exhibits selective cytotoxicity toward senescent cells, specifically inhibiting the activity of etoposide-induced senescent IMR-90 cells with an IC50 of 10.7 μM. Additionally, BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21, and KI67 in aged mouse models.

TFCP2L1-IN-1 is a TFCP2L1 transcription factor inhibitor that regulates cell proliferation and promotes antitumor effect of Sorafenib by STAT3/NANOG pathway.

<p>p53 Activator 14 (Compound 7A) is a derivative of Neratinib that can induce DNA damage and activate p53, thereby inhibiting the proliferation of various cancer cells, with an IC50 of 7.21 μM for HCT116 cells. This compound hinders adhesion, migration, and invasion of HCT116 cells, disrupts the cell cycle, and triggers apoptosis. In addition, p53 Activator 14 exhibits anti-tumor properties and inhibits angiogenesis in the chick embryo chorioallantoic membrane (CAM) model.</p>

<p>HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.</p>

<p>TBC-1 is a chlorophyll-a derivative that acts as a photosensitizer for photodynamic therapy (PDT). It efficiently generates type I ROS and targets the endoplasmic reticulum. TBC-1 demonstrates in vitro biocompatibility and PDT effectiveness under both normoxic and hypoxic conditions.</p>

Elocalcitol is a calcitriol analog for inhibition of prostate cell growth.

<p>HDAC-IN-81 (Compound 11g) is an HDAC inhibitor capable of effectively inhibiting HDAC1 with an IC50 value of 4.5 nM. Additionally, it exhibits anticancer activity by inhibiting cell proliferation and can induce cell apoptosis (apoptosis).</p>

TLBC, a borane-chalcone derivative, exhibits dose-dependent inhibitory effects across various glioma cell lines with IC50 values ranging from 5.5 to 25.5 μM. TLBC induces apoptosis independently of alterations in the tumor suppressor factor p53.

TP-030-1, RIPK1 inhibitor: K(i) hRIPK1 at 3.9nM, IC50 mRIPK1 at 4.2μM; targets inflammation, neurodegeneration research.

Antiproliferative agent-63 (compound 4d) is a cyclic analog of cannabidiol that acts as an anticancer agent. It demonstrates favorable activity against breast and colorectal cancer. Moreover, this compound can arrest the cell cycle in the G1 phase and induce apoptosis through the mitochondrial pathway in breast cancer cell lines.

Nitrovin is an antimicrobial growth promoter that induces ROS-mediated non-apoptotic and quasi-apoptotic cell death by targeting TrxR1. It exhibits anticancer activity with IC50 values ranging from 1.31 to 6.60 μM for both tumor and normal cells.

Triphen diol, a phenol diol, fights pancreatic cancer & cholangiocarcinoma, inducing apoptosis via caspase-dependent & -independent paths.

Utibaprilat is the primary degradation product of Utibapril and functions as an ACE inhibitor.

06:0 PE (PE(6:0/6:0)) is a water-soluble phospholipid characterized by its short acyl chains. It possesses notable antitumor activity and can inhibit tumor progression in the body. Additionally, it exhibits antiproliferative and pro-apoptotic properties, and serves as a precursor for phosphatidylcholine and phosphatidylethanolamine.

Anticancer agent 16 showed good cytotoxic effects on HCT-116 cell line (IC50: 8.55 μM), NCI-H460 cell line (IC50: 5.41 μM) and SKOV3 cell line (IC50: 6.4 μM).

<p>HAC-Y6 exerts its anticancer effects by inducing cell cycle arrest. It prompts apoptosis in COLO 205 cells with an IC50 of 0.52 µM.</p>

PBX-7011, an active camptothecin derivative, binds to the DDX5 protein in cells and induces cell death through DDX5 protein degradation [1].

Antitumor Agent-100 (compound A6) is a molecular gel and apoptosis inducer targeting PDE3A-SLFN12 with an IC50 of 0.3 μM, demonstrating potent antitumor activity. This orally available agent binds to the PDE3A enzyme pocket, recruiting and stabilizing SLFN12 which disrupts protein translation and induces apoptosis [1].

<p>RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.</p>

FKBP51-Hsp90-IN-2 (Compound E08) functions as a selective inhibitor for the FKBP51 - Hsp90 protein-protein interaction, exhibiting IC 50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. Beyond its inhibitory actions, FKBP51-Hsp90-IN-2 enhances cellular energy metabolism and promotes neurite growth. This compound is utilized in the study of neurodegenerative diseases and cancer [1].

JAK2/FLT3-IN-1 (TFA), an oral JAK2/FLT3 inhibitor, shows anticancer properties; IC50: JAK2 (0.7 nM), FLT3 (4 nM), JAK1 (26 nM), JAK3 (39 nM).

YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that disrupts the interaction between YAP/TAZ and TEAD. It inhibits the transcriptional activity of TEAD with an IC50 of 1.2 nM. Additionally, YAP/TAZ-TEAD-IN-2 suppresses the expression of target genes (Cyr61, CTGF, AXL, and Survivin) and the proliferation of breast cancer cells.

Antitumor agent-43 (Compound 4B) is a potent antitumor agent that induces cell cycle arrest at G2/M phase.

Antibacterialagent 254 (Compound 2) is an antimicrobial agent capable of eradicating 7-day-old P. aeruginosa biofilms at a concentration of 50 μM without affecting bacterial growth. Additionally, Antibacterialagent 254 enhances the efficacy of Ciprofloxacin against P. aeruginosa and upregulates the expression of the matrix-degrading enzyme genes pelA, pslG, and eddA.

RET-IN-10: Potent RET inhibitor, may treat congenital megacolon and tumors (Patent WO2021135938A1, compound 18).

Pan-Trk-IN-3: potent Trk inhibitor (IC50: 2-26 nM), effective against drug-resistant mutants, induces apoptosis, anti-tumor effects.

VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

TNF-α-IN-2 is orally active TNFα inhibitor that distorts the TNFα trimer, causing abnormal signal transduction when it binds to TNFR1, rheumatoid arthritis.

SF-9-2 is a PD-L1/PD-1 binding inhibitor with an IC50 of 24.9 nM. It suppresses epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, while also inducing apoptosis and causing cell cycle arrest. SF-9-2 blocks PD-L1-induced growth of SK-N-SH cells via the MAPK signaling pathway. It restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. In the SK-N-SH NOG mouse model, SF-9-2 inhibits tumor growth without notable toxicity. Additionally, SF-9-2 acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function and is applicable to neuroblastoma research.

sEH-IN-21 is an orally active inhibitor of sEH, exhibiting IC50 values of 0.1 nM for both hsEH and msEH. It significantly suppresses the NF-κB signaling pathway. sEH-IN-21 demonstrates potent anti-inflammatory activity by reducing IL-6 and TNF-α release and maintaining intestinal barrier integrity. It is applicable in research on inflammatory bowel disease (IBD).

Neral, a monoterpenoid compound, exhibits anti-inflammatory and anticancer activities. It inhibits TNF-α and IL-6, along with inflammatory mediators such as pro-IL-1β, iNOS, COX-2, and NLRP-3.

ST-899 is an innovative platelet-activating factor (PAF) receptor antagonist. It significantly reduces the mortality rate in mice experiencing shock induced by endotoxins (LPS). The compound markedly inhibits the LPS-induced increase in serum tumor necrosis factor (TNF) levels while leaving interleukin-6 (IL-6) unaffected. The mechanism by which ST-899 operates involves disrupting the positive feedback loop between PAF and TNF, thereby mitigating inflammatory responses. ST-899 is applicable for studies related to inflammatory diseases such as septic shock.

RIPK2-IN-6 (Compound 15a) is an inhibitor of RIPK that specifically targets the phosphorylation of RIPK2, thereby suppressing the NF-κB and MAPK signaling pathways. It has demonstrated anti-inflammatory and anti-fibrotic activities in a mouse model of colitis induced by Dextran sodium sulfate.

Hdm2 E3ligaseinhibitor 1 (Compound 1) is a reversible inhibitor of Hdm2-mediated p53 protein ubiquitination, with an IC50 of 12.7 μM. It binds to Hdm2, blocking the transfer of ubiquitin catalyzed by Hdm2 from pre-linked Ub-Ubc4 to p53, thereby inhibiting p53 ubiquitination, stabilizing p53 protein in tumor cells, and exerting antitumor activity.

MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. It selectively inhibits MAO-B with an IC50 of 87.47 nM, demonstrating a selectivity over MAO-A by more than 229 times. In vitro, MAO-B-IN-45 exhibits significant anti-ferroptosis activity by modulating iron metabolism pathways and the GSH-GPX4 axis. Additionally, it improves cognitive and behavioral deficits in 3×Tg (APP/Tau/Ps1) Alzheimer's disease mice and significantly reduces levels of ferritin heavy chain 1 (FTH1), β-amyloid protein (APP), and Tau protein phosphorylation (p-Tau) in their brains.

LLW-018 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 2.61 nM. It can disrupt the PD-1/PD-L1 interaction, with a cell-based PD-1/PD-L1 blocking bioassay IC50 value of 0.88 μM. LLW-018 holds potential for research in immune-related diseases.

Anticancer agent 17 was effective against HeLa cells (IC50: 0.19 μM) and A2780 cells (IC50: 0.09 μM).

GlcNAc-MurNAc is a disaccharide and mild TLR4 agonist with a Kd of 383 μM for mouse TLR4. It directly binds to TLR4, activating the downstream NF-κB and IRF pathways. Additionally, GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice through a TLR4-dependent mechanism, making it useful for inflammatory bowel disease research.

FLT3-IN-32 is a potent FLT3 inhibitor with high selectivity, effectively suppressing FLT3 activating mutations and inducing apoptosis. It demonstrates good tolerance in non-tumor-bearing mice. In NOD/SCID mice loaded with MV4-11 cells, FLT3-IN-32 exhibits outstanding antitumor efficacy, significantly extending mouse survival. FLT3-IN-32 is applicable for acute myeloid leukemia research.

MAPK-IN-5 is a potent inhibitor of MAPK, with an IC50 value of 1.35 μM in HeLa cells. It induces ROS-mediated DNA damage and mitochondrial apoptosis (apoptosis) via the MAPK pathway. MAPK-IN-5 significantly inhibits colony formation in HeLa cells, reduces viable cell numbers, suppresses cell migration, and arrests the cell cycle at the G2/M phase. It is applicable in cervical cancer research.

Z-VAD-AMC acts as a substrate specifically for caspase-9.

6:2 Cl-PFAES exhibits reproductive toxicity by elevating the levels of serum estradiol and vitellogenin in adult males, which can harm the embryonic development of offspring.

ASK1ligand 1 is a binding ligand for ASK1 and can be utilized to synthesize PROTACs such as dASK1-VHL.

INNO-220 is an orally active, CRBN-dependent molecular glue degrader that targets CK1α. By degrading CK1α, INNO-220 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis (Apoptosis). It disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, inhibiting the NF-κB signaling pathway in T cells and lymphoma cells with activating mutations in CARD11. INNO-220 offers a novel direction for lymphoma research.

<p>TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.</p>

Nampt-IN-16 (Compound 9a) is an orally active NAMPT inhibitor with an IC50 of 0.15 μM. It reduces intracellular NAD+ and ATP levels. Nampt-IN-16 inhibits the proliferation, migration, and invasion of gastric cancer cells, induces cell cycle arrest and apoptosis, and alters cellular metabolism. This compound is applicable for research in tumors such as gastric cancer.

Minnelide treats pancreatic cancer, hinders androgen-related prostate growth, shrinks tumors, and improves survival.

NPB-1575 is a potent, orally active anti-inflammatory agent capable of crossing the blood-brain barrier. It mitigates neuroinflammation and resists ferroptosis by activating IRS2/Nrf2/NF-κB. NPB-1575 protects against cerebral ischemic injury and improves neurological function outcomes, making it suitable for research in focal ischemic stroke.

UR-AK49 (compound 11) is an agonist for the human histamine H1 and H2 receptors. It exhibits an EC50 of 23 nM in the GTPase assay involving hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 is applicable in neurologically related research.

<p>HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.</p>

Aplysin suppresses breast cancer cells and protects liver cells by blocking PI3K/AKT/FOXO3a and preventing oxidative damage.

Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the suppressive effects of Cyclophosphamide in animal models of rat adjuvant arthritis and mouse collagen-induced arthritis.

LRRK2-IN-17 is an orally active LRRK2 inhibitor with IC50 values of 3.5 nM for WT and 3.3 nM for G2019S, and it also inhibits RET kinase with an IC50 of 59 nM. LRRK2-IN-17 is utilized in research related to cancer and Parkinson's disease (PD).

t9,t11,c15-CLNA is an isomer of conjugated linolenic acid (CLNA) produced by Lactobacillus plantarum ZS2058. It exhibits key activities including anti-inflammatory and antioxidant effects, as well as enhancement of intestinal barrier function. The regulatory mechanisms of t9,t11,c15-CLNA involve the upregulation of tight junction proteins, the inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6), and the activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be utilized in research on inflammatory bowel disease (like colitis).