Apoptose

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

Anagrelide HCl monohydrate is a platelet-reducing imidazoquinazoline for ET and PV research.

Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].

Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.

WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.

Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.

ASR-488, an activator of the mRNA-binding protein CPEB1, promotes apoptosis and suppresses the growth of bladder cancer [1].

TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.

MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and

Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.

A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle

PD-L1/CD-73-IN-1 (compound CC-5) is an inhibitor of PD-L1 and CD73, with IC50 values of 6 nM and 0.773 μM, respectively. It effectively inhibits tumor cell growth both in vitro and in vivo.

UZH1a: METTL3 inhibitor, IC50 280 nM, used for epitranscriptomic modulation and has antitumor properties.

RA-XII is a useful organic compound for research related to life sciences. The catalog number is T125868 and the CAS number is 143343-98-0.

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

CQ1373 is a potent RET inhibitor that demonstrates cellular activity against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C, and CCDC6-RET-G810R, with IC50 values of 13.0, 25.7, and 28.4 nM, respectively. It shows excellent selectivity for wild-type RET and solvent front mutants G810C/R, with IC50 values of 4.2, 7.1, and 32.4 nM. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. Additionally, it induces apoptosis (Apoptosis) and cell cycle arrest in BaF3 cells. CQ1373 possesses antitumor efficacy, making it a candidate for cancer research.

UAMC-4821 is a ferroptosis inhibitor with an IC50 of 5.2 nM. It effectively scavenges free radicals, inhibits lipid peroxidation, and prevents ML162-induced ferroptosis, providing protective effects on HT-1080 cells. With favorable pharmacokinetic properties in mice, UAMC-4821 presents an oral bioavailability of 63% and demonstrates blood-brain barrier permeability.

Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.

1D09C3 is a fully humanized anti-HLA-DR monoclonal antibody. It induces cell apoptosis (apoptosis) and death through a cascade of reactions, including reactive oxygen species (ROS) production, JNK activation, mitochondrial membrane depolarization, and the release of AIF from mitochondria. In xenograft models with JVM-2 cells and GRANTA-519 cells in mice, 1D09C3 demonstrated significant antitumor activity, improving overall survival and median survival time. This compound is applicable in cancer research, including studies on chronic lymphocytic leukemia (CLL).

Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.

OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.

[1,1'-Biphenyl]-3-amine is an inhibitor of MAO-A and MAO-B and can inhibit the cell viability of HT-29, HEK 293, and MCF-7 cells.

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

C199 is a PROTAC degrader targeting PRMT4 with a DC50 of 106 nM. It demonstrates high selectivity for PRMT4 compared to other protein arginine methyltransferases. C199 exhibits strong cellular degradation capacity and induces apoptosis in multiple myeloma cell lines. It efficiently eliminates PRMT4 protein through the VHL-proteasome pathway. C199 has a relatively long half-life and shows potent anti-multiple myeloma (MM) activity.

Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.

Milademetan tosylate hydrate, an oral MDM2 inhibitor targeting AML and solid tumors, induces G1 arrest and apoptosis.

Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.

HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells.

HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.

Varlilumab (CDX-1127) is a novel human IgG1 anti-CD27 monoclonal antibody. Varlilumab has antitumor activity and can be used to study advanced solid tumors.

YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.

Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

3-Hydroxykynurenine (3-hydroxy-DL-Kynurenine) is an active metabolite of tryptophan and inhibits yeast and rat liver aldehyde dehydrogenase by 97 and 69%.

MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.

Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.

Photosensitizer-6 (Compound 4) is a metal ion complex that inhibits TrxR. It induces apoptosis in 4T1 cells, targeting cancer cells and eliminating tumors through chemophototherapy and immunogenic cell death under illumination. Additionally, Photosensitizer-6 can be utilized for tumor imaging.

BRD4/FKBP12 degrader-1 (a1d) is an anticancer agent that functions as a BRD4/FKBP12 degrader.

CS4 is a selective HDAC inhibitor, with IC50 values for HDAC1, HDAC6, HDAC8, HDAC4, and HDAC11 reported as 38 nM, 12 nM, 5.8 μM, 19 μM, and 61 μM, respectively. It enhances the acetylation of α-tubulin and histone 3 (histone 3). Additionally, CS4 activates PPARγ and blocks glycolysis (glycolysis). It induces cell cycle arrest at the G2 phase and triggers apoptosis (apoptosis), exhibiting anticancer effects both in vitro and in vivo.

PD1-PDL1-IN 1 TFA (compound 16) is a potent inhibitor of programmed cell death 1 (PD-1), functioning as an immune modulator [1].

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

RK-10 is a peptide that binds to PD-L1. After being conjugated with Cy5 or Biotin, RK-10 can be used to identify PD-L1-expressing tumors through flow cytometry or immunohistochemistry. It is applicable for research in detecting cancers such as non-small cell lung cancer (NSCLC), breast cancer, squamous cell carcinoma, and melanoma.

Bromoiodoacetamide (I-HAcAm): cytotoxic, induces ROS & apoptosis in HepG-2 cells.

Thalidomide-NH-PEG2-COOH: a synthesized E3 ligase ligand-linker with cereblon ligand and PROTAC linker.

eIF4A3-IN-7: Potent eIF4A3 inhibitor, potential cancer/dysproliferation research (WO2019161345A1, Compound 8).

RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.

S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is effective against BCL-2 mutations, including G101V and D103Y.

Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.

Xylopine: an aporphine alkaloid, cytotoxic to cancer cells, induces oxidative stress, G2/M arrest, and apoptosis.

eIF4E-IN-1 inhibits eIF4E and boosts immunity by targeting PD-1, PD-L1, LAG3, TIM3, IDO, aiding cancer and infection treatment.

RIPK2-IN-2, a RIP2 kinase PROTAC inhibitor, blocks proinflammatory signaling in autoinflammatory diseases.

Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.

DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.

GPX4-IN-6 is a GPX4 inhibitor with antitumor activity.GPX4-IN-6 induces iron death and is used for the treatment and prevention of triple-negative breast cancer

SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.

(Rac)-BIO8898 is a chemical compound that serves as an inhibitor of the co-stimulatory interaction between CD40 and CD154.

Anticancer agent 104 has anticancer activity, and induces cancer cell apoptosis [1] .

STAT3-IN-40 (Compound 8b) is an anticancer agent. It initiates immune responses in CD4+ and CD8+ T lymphocytes by inhibiting the expression and phosphorylation of STAT3, and induces ferroptosis and apoptosis in tumor cells. STAT3-IN-40 is valuable for research into cancer chemoimmunotherapy drugs.

TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, showing significant antiproliferative activity. It can induce G1 phase cell cycle arrest and apoptosis (with notable increases in early and late apoptosis rates) and is useful for research in cancers such as colon, breast, and liver cancer.

Fludarabine triphosphate inhibits key enzymes, causing cell death.

D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1/Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.

STAT3/NF-κB-IN-1 is a potent inhibitor of STAT3 and NF-κB, exhibiting IC50 values of 5.86 μM for STAT3 and 4.22 μM for NF-κB in 4 T1 cells. It induces apoptosis by upregulating key apoptotic regulators (caspases-3, 9, Bax) and downregulating Bcl-2 expression. STAT3/NF-κB-IN-1 shows significant anticancer activity against breast cancer cell lines and can reduce tumor volume in vivo. It is applicable for research in breast cancer.

Pimagedine is a prototype therapeutic agent for the prevention of formation of advanced glycation endproducts.

Antitumor Agent-64 (Compound 8d), a diosgenin derivative, exhibits potent cytotoxic activity against the A549 cell line and induces apoptosis in A549 cells

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

Calphostin C is a protein kinase C inhibitor.

β-ESA, a polyunsaturated fatty acid in seed oils, inhibits Caco-2 cell growth dose- and time-dependently.

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.

TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.

Gamgertamig is a humanized bispecific antibody of the IgG4 type that targets TNFRSF17 and CD3E.

Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.

Thalidomide-O-C4-COOH is a synthetic E3 ligase linker derived from Thalidomide for PROTAC tech.

Dehydroaltenusin is a selective eukaryotic DNA polymerase α inhibitor and a type of antibiotic produced by a fungus (IC50: 0.68 μM).

NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.

E3 ligase Ligand 36 is an E3 ligase ligand that can be utilized for synthesizing PROTACs, such as PROTAC BRM/BRG1 degrader-1.

Chalcones A-N-5, a non-cytotoxic trihydroxy chalcone, aids cell growth & neuroprotection, inhibits ferroptosis, and targets AD research.

KP1019 is now discontinued.

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080

LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.

VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.

PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density

2,2'-Dihydroxy chalcone inhibits β-glucuronidase (IC50=1.6 μM) and lysozyme (IC50=1.4 μM), and fights E. coli, S. fowleri, S. albicans, S. aureus.

Pyridinium bisretinoid A2E (A2E) is a fluorescent molecule isolated from the lipofuscin of retinal pigment epithelium, a weak photosensitizer.

ERK1/2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.

FMP is a platinum (IV) complex. It significantly upregulates the expression of γ-H2AX and p53, enhances ROS production, and markedly increases the expression of apoptosis (Apoptosis) related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP exhibits antiproliferative activity against breast cancer.

SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and

Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.

PNT100: 24-base DNA oligo targeting BCL-2 regulatory region; halts tumor cell growth, induces death.

Cardanol (C15:1), found in cashew nut shell liquid, induces mitochondria-associated apoptosis in human melanoma cells.

HX009 is a bispecific antibody that targets PD1 and CD47, though its binding to CD47 is attenuated. HX009 functions by blocking PD1/CD47 and can be utilized in research related to non-Hodgkin lymphoma (NHL).

eIF4E-IN-5 (Compound 6n) is a cell-permeable eIF4E inhibitor that binds to capped mRNA, thereby inhibiting cap-dependent translation [1].

Asudemotide is a bioactive chemical.