Apoptose

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

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.

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

(±)-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.

Antitumor agent-76 is a water-soluble, orally active, rapid-release prodrug of Triptolide that exhibits anticancer effects.

HSP90-IN-10 is a potent HSP90 inhibitor, targeting HCC1954 cells (IC50: 6 μM) and inducing apoptosis, sparing normal cells.

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.

APD-94 is a dual inhibitor targeting tubulin and Bmi-1. It disrupts the normal polymerization of tubulin and suppresses the expression of Bmi-1. This compound induces cell cycle arrest at the G2/M phase and triggers apoptosis, thereby inhibiting cancer cell proliferation. Additionally, APD-94 inhibits the growth of HT29 cell xenograft tumors in NOD/SCID mice and is applicable to colorectal cancer research.

LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of

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.

HP590: potent oral STAT3 inhibitor, IC50=27.8 nM, blocks ATP, IC50=24.7 nM, hinders gastric cancer growth, triggers cell death.

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.

Ferroptosis-IN-18 (51) is a phenothiazine derivative known for its potent anti-ferroptotic and antioxidant properties. It is useful for research related to intracerebral hemorrhage (ICH).

STAT3-IN-9 hinders STAT3 at Tyr705, doesn't affect STAT1 Tyr701, induces apoptosis, and arrests cells in G2/M phase.

A signal-specific JNK/p38 pathway and TAK 1 inhibitor

ZLWT-37: Oral CDK inhibitor, CDK9 IC50=0.002 µM, CDK2 IC50=0.054 µM; halts HCT116 cells at G2/M, induces apoptosis.

Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.

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.

IMB5046 is a microtubule inhibitor that induces apoptosis (cell death) by obstructing the G2/M phase of the cell cycle. It possesses antitumor properties.

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value

MRK003, a γ-secretase inhibitor, induces apoptosis, halts cell growth in myeloma/NHL, and affects notch signaling and PI3K/Akt pathway.

EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.

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.

VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.

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.

MNK1/2-IN-6: Strong, selective MNK1/2 inhibitor; IC50s: MNK1 at 2.3 nM, MNK2 at 3.4 nM; triggers dose-dependent apoptosis.

HER2-IN-10 is a psoralen derivative that induces apoptosis. HER2-IN-10 shows anti-breast cancer activity and light-activated cytotoxicity [1].

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.

Tubulin polymerization-IN-4: inhibits tubulin (IC50=4.6 μM), blocks G2/M phase, induces apoptosis, hinders cell cloning/migration, damages vasculature.

Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. It induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, while decreasing GPX4 protein expression. Nur77 agonist-1 binds with affinity to the ligand binding domain of Nur77, with a KD of 13.80 μM. It demonstrates significant antiproliferative activity against various breast cancer cells (IC50: 2.15-3.26 μM) and exhibits low cytotoxicity towards normal cells. This compound is useful for breast cancer research.

YK5 is an allosteric inhibitor pocket of Hsp70 and represents a previously unknown chemical tool to investigate cellular mechanisms associated with Hsp70.

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.

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.

Antiproliferative agent-4 suppresses cancer cell growth with low toxicity, inhibits tumors in mice, and induces apoptosis in EC109 cells.

Thalidomide-NH-amido-PEG2-C2-NH2 is a synthetic E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. It is utilized in the synthesis of PROTACs.

Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].

KMUP-1 is a xanthine derivative known for its vasodilatory properties. It functions as a phosphodiesterase (PDE) inhibitor and an activator of soluble guanylate cyclase (sGC), engaging the NO/sGC/cyclic guanosine monophosphate pathway. Additionally, KMUP-1 can open K+ channels and has the potential to alleviate ischemia-induced cardiac myocyte apoptosis (apoptosis). This compound is useful in cardiovascular and anti-inflammatory research.

Isoforretin A is a potent inhibitor of thioredoxin-1 (Trx1) with significant biological activity, inducing anti-tumor effects mediated by reactive oxygen species (ROS). The compound inhibits Trx1 activity by covalently binding to the activation site residues Cys32/Cys35, which triggers ROS accumulation, leading to DNA damage and apoptosis (Apoptosis) in cancer cells. Additionally, Isoforretin A has demonstrated the ability to suppress the growth of HepG2 tumors in a mouse hepatic cell carcinoma xenograft model.

Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.

SC428 acts as an inhibitor of the androgen receptor (AR), specifically targeting the N-terminal domain of AR. This compound effectively diminishes the transactivation of various AR forms, including AR-V7, ARv567es, full-length AR (AR-FL), and its LBD mutants. Additionally, SC428 significantly inhibits AR-FL nuclear translocation, chromatin binding, and AR-regulated gene transcription under androgen stimulation. In vitro, SC428 suppresses the proliferation of tumor cells. In vivo, it inhibits tumor growth in mice transplanted with 22Rv1 cells by inducing apoptosis.

GGTI298 is a potent GGTase I inhibitor; IC50 3μM for Rap1A, >20μM for Ha-Ras.

SIJ1777, a derivative of GNF-7, exhibits potent anticancer effects against melanoma cells harboring BRAFI/II/III mutations. The compound significantly inhibits the activation of MEK, ERK, and AKT. Furthermore, SIJ1777 notably induces apoptosis (cell death) and effectively prevents migration, invasion, and anchorage-independent growth of melanoma cells with BRAFI/II/III mutations.

NSD2-IN-1: potent, selective NSD2-PWWP1 inhibitor, IC50 0.11 μM, induces gene expression changes, apoptosis, cell cycle arrest.

PD-1/PD-L1-IN-17 (Compound P20) is a potent PD-1/PD-L1 inhibitor (IC50: 26.8 nM).

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).

EGFR-IN-45: Strong EGFR/CDK2 inhibitor (IC50s: 0.4 & 1.6 μM), halts cancer cell cycle pre-G1, prompts apoptosis, also targets Topo I/II.

HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.

Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTAC.

PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).

AZD0424: oral Src/Abl kinase inhibitor; potential anticancer; induces apoptosis, cell cycle arrest in lymphoma.

FLT3-ITD-IN-3 (13v) is an orally active inhibitor of FLT3-ITD (internal tandem duplication of FLT3), which works by blocking FLT3 signaling. This inhibition leads to cell cycle arrest in the G0/G1 phase and induces apoptosis. The compound is currently employed in studies related to acute myeloid leukemia (AML).

Topoisomerase I/II inhibitor 4 halts cell growth and spread, induces apoptosis, and is used in liver cancer research.

HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).

MI-888 (TFA) is an orally active inhibitor of the MDM2-p53 interaction with a Ki of 0.44 nM. It can induce rapid, complete, and durable tumor regression in xenograft mouse models.

2-Deoxy-L-ribose is the stereoisomer of 2-Deoxy-D-ribose and can inhibit the anti-apoptotic effects of 2-Deoxy-D-ribose. Additionally, 2-Deoxy-L-ribose is capable of suppressing tumor cell metastasis by downregulating thymidine phosphorylase overexpression.

ISR Modulator-1 (Compound 212) acts as a regulator for the integrated stress response pathway (ISR).

DHU-Se1: potent anti-inflammatory, releases reactive selenium from macrophages, inhibits iNOS/TNF-α, blocks M0 to M1 polarization.

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.

(R)-SL18 is a degrader of ANXA3 that facilitates its breakdown via ubiquitination. This compound can inhibit the proliferation, migration, invasion, and colony formation of breast cancer cells, while also inducing apoptosis. (R)-SL18 is applicable for research in triple-negative breast cancer.

MD102, with an IC50 value of 0.35 μM, is a potent TG2 inhibitor that stabilizes p53 by inhibiting TG2. This results in a decrease in p-AKT and p-mTOR downstream signaling, ultimately inducing tumor cell apoptosis [1].

PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual inhibitor targeting PD-L1 and VISTA. It effectively hinders the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), leading to the reactivation of T cells. Additionally, PD-L1/VISTA-IN-1 exhibits antitumor activity.

MGD-22 is a molecular glue and orally active degrader of IKZF1/2/3, with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. It exhibits strong anti-proliferative activity against various hematological cancer cells and induces cell apoptosis (apoptosis). MGD-22 demonstrates significant anti-tumor efficacy in mice with NCI-H929 or WSU-DLCL-2 xenografts. This compound is useful for researching blood cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).

SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. It effectively suppresses the expression of SIRT1, SIRT2, and SIRT3, leading to increased acetylation and activation of p53. Additionally, SIRT-IN-7 inhibits the proliferation of breast cancer cells and induces apoptosis and autophagy, demonstrating antitumor activity.

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.

PKM2 modulator 2 (compound C599) is a potent inhibitor of PKM2, displaying antiproliferative activity and inducing apoptosis. This compound holds potential for research in glioblastoma.

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.

DDO-8958 is an orally active and selective BET BD1 inhibitor, exhibiting a KD of 5.6 nM for BRD4 BD1. It shows low nanomolar inhibitory activity across all BET BD1 bromodomains except for BRDT BD1. DDO-8958 inhibits tumor cell proliferation and migration, induces apoptosis and cell cycle arrest, and demonstrates antitumor activity.

SSB-2548 is a CXCR-4 inhibitor that suppresses the proliferation and migration of acute myeloid leukemia cells and induces apoptosis (apoptosis). It is well absorbed in the gastrointestinal tract and can be used for leukemia research.

MG28 exhibits significant cytotoxic effects, likely stemming from its direct and potent DNA-damaging activity. The compound is utilized in cancer research.

PD-L1/HDAC6-IN-1 (Compound HP29) is an inhibitor targeting both PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction and inhibiting HDAC6 activity, with IC50 values of 26.8 nM and 69 nM, respectively. This compound enhances the cytotoxicity of Jurkat T cells against HepG2 cells, exhibiting an IC50 of 3.4 μM. In rats, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics, showing a drug exposure level of 871.62 ng·h/mL, and displays antitumor activity in a B16-F10 xenograft mouse model.

Apoptosisinducer 36 (Compound 42) exhibits anti-leukemic activity by reducing leukemia stem cells (LSC) and inducing differentiation. It inhibits proliferation of AML cells by causing cell cycle arrest in the G1 phase, and induces PANoptosis, which includes apoptosis, pyroptosis, and necrosis.

EMT inhibitor-3 (compound 11i) is an epithelial-mesenchymal transition (EMT) inhibitor that effectively suppresses the proliferation, migration, and invasion of SK-N-SH neuroblastoma cells, with an IC50 value of 2.5 μM. It induces mitochondrial-mediated intrinsic apoptosis in tumor cells by enhancing the Bax/Bcl-2 protein expression ratio, promoting the release of cytochrome C from mitochondria, and activating caspase 9 and caspase 3. EMT inhibitor-3 is applicable for cancer research.

WB436B, a highly selective STAT3 inhibitor, effectively targets and inhibits STAT3-Tyr705 phosphorylation along with the expression of STAT3 target genes. It exhibits cytotoxic effects on pancreatic cancer cells by inducing apoptosis. Furthermore, WB436B suppresses tumor growth and metastasis in pancreatic cancer mouse models, thereby prolonging the survival of tumor-bearing mice.

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

GPX4 Activator 2 (Compound C3) serves as an activator of GPX4 and exhibits cardioprotective effects by inhibiting cellular iron death (ferroptosis) with an efficacy concentration (EC50) of 7.8 μM. It is used in the study of myocardial damage.

ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.

TZEP7 functions as an EGFR kinase inhibitor in cancer cells. It exhibits cytotoxicity and induces apoptosis within these cells. TZEP7 downregulates the anti-apoptotic protein Bcl-2, upregulates the pro-apoptotic protein Bax, and increases caspase levels. This compound holds potential for research in anticancer drug development.

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

RET-IN-1 is a RET kinase inhibitor (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively).

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.

PF-7006, an Mps1 kinase inhibitor, exhibits a Ki value of 0.27 nM and an IC50 value of 2.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reduces histone H3 levels, and shortens the duration of mitosis, thereby inducing apoptosis (Apoptosis) in cancer cells. When used in combination with Palbociclib, the tolerance of cancer cells to PF-7006 is enhanced. PF-7006 is applicable for research on breast cancer.

PARP10/15-IN-2 (Compound 8h) blocks PARP10/15, has IC50s: 0.15μM/0.37μM, cell-permeable, prevents apoptosis.

Potent oral XIAP/cIAP1 inhibitor with EC50s: XIAP 5.1 nM, cIAP1 0.32 nM; curbs tumor growth in vivo.

Topoisomerase I/II inhibitor 3 suppresses cell growth and induces apoptosis in liver cancer by blocking PI3K/Akt/mTOR.

Metamizole (Dipyrone) hemimagnesium is an anti-inflammatory and antioxidant compound known for its ability to reduce fever. It decreases levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Additionally, Metamizole hemimagnesium acts as an orally active cyclooxygenase (COX) inhibitor, suppressing cell proliferation and promoting apoptosis. It is utilized in the study of inflammation and fever.

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.

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.

Decarbamoylmitomycin C, an analog of Mitomycin C (MC), functions as a DNA alkylating agent. It is capable of activating chromatin relaxation by the ataxia-telangiectasia and Rad3-related protein (ATR) in a p53-independent manner.

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

[D-Leu-4]-OB3 suppresses the expression of genes associated with inflammation, proliferation, and metastasis, as well as the expression of PD-L1.

KIRA9 inhibits IRE1 with a 4.8 μM IC50, blocking ER-stress-induced mRNA decay and apoptosis by fully binding IRE1's ATP site.

MC3629, an inhibitor of the histone methyltransferase (EZH2), exhibits antitumor activity. This compound effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while inducing cell apoptosis (apoptosis). MC3629 is also useful in research on tumor aggressiveness and resistance.

PLK1-IN-13 is a selective, orally active PLK1 inhibitor with an IC50 of 0.27 nM. It also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 induces cell cycle arrest at the G2 phase, promotes apoptosis, and downregulates the transcription of the cancer-associated oncogene c-MYC. This compound inhibits tumor growth and is applicable for research in acute myeloid leukemia (AML).

(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) sodium is a synthetic derivative of oleic acid (OA) that binds to the plasma membrane, altering lipid composition. This compound exhibits antitumor properties.

Compound 28 is a nonsteroidal VDR agonist with 690 nM potency, inducing cell cycle arrest and apoptosis in MCF-7 cells.

c-Myc inhibitor16 iodide (Compound W11) is a selective inhibitor of the c-MycG-quadruplex (c-MycG4). It suppresses the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle by halting growth at the G0/G1 phase, and activates mitochondrial apoptotic pathways, leading to early apoptosis in cancer cells. This compound shows potential for research in breast cancer.

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).