Apoptose

SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.

SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti

Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC) with IC50 values of 4

2-Chlorophenoxazine is an Akt inhibitor that demonstrates an in vitro inhibitory concentration (IC50) of 2-5 μM and has the capacity to induce apoptosis.

Bcl-2-IN-16 is a Bcl-2 (B-cell lymphoma 2) inhibitor [1].

Photosensitizer-2 (compound 1), an organic D-π-A sensitizer, exhibits antitumor properties and potent phototoxicity due to an acrylic acid moiety.

PLK1-IN-4 is a selective PLK1 inhibitor, antiproliferative , induces cell cycle arrest and apoptosis, making it suitable for hepatocellular carcinoma research.

HDAC-IN-53 inhibits HDAC1-3 with IC50s: 47, 125, 450 nM. Inactive on class II HDACs; triggers apoptosis; reduces tumor growth in mice.

CDKI-83, a potent CDK9 inhibitor, inhibits tumor growth with GI50 <1μM and triggers apoptosis in A2780 cells, showing promise as an anti-cancer agent.

Mezigdomide (CC-92480) is a potent, novel cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue.Cost-effective and quality-assured.

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.

NF 023 is a potent, selective P2X1 purinoceptor antagonist.

Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces

GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively

Docebenone is a selective and orally active inhibitor of 5-LO.

HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1.

HJC0152 (free base) is an orally active, potent STAT3 inhibitor that impedes cell cycle progression, induces apoptosis, and notably reduces MDA-MB-231 xenograft

NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1,IC50 = 14 nM). The IC50 value for ASK2 is 0.51 μM.

CPT-Se4, a seleno-derivative of CPT, effectively kills cancer cells, triggers apoptosis, and is cytotoxic against various cell lines.

1,2-Di-13(Z)-docosenoyl-3-oleoyl-rac-glycerol is a triacylglycerol composed of 13(Z)-docosenoic acid at both the sn-1 and sn-2 positions and oleic acid at the sn-3 position.

AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.

Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.

Compound D16 (Anticancer agent 168) is an inhibitor of DNA2 that induces apoptosis and cell-cycle arrest predominantly in the S-phase.

(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 μM, respectively).

Cis-3,4',5-Trimethoxy-3'-hydroxystilbene, a stilbene derivative, induces apoptosis through the mitochondrial release of cytochrome c and suppresses tubulin polymerization. It is also noted for its application in leukemic research [1].

eIF4A3-IN-17, a silvestrol analogue, disrupts eIF4F assembly; EC50: 0.9-15 nM. Used in cancer pathogenesis research.

RIPK1-IN-8 is an aminoimidazolopyridine and is a selective and potent inhibitor of RIPK1 (IC50: 4 nM).RIPK1-IN-8 has research potential in inflammatory diseases

HM90822 is an IAP antagonist that inhibits XIAP and cIAP1/2 protein expression, induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.

JAB-2485 is a highly potent and selective inhibitor of Aurora kinase A (AURKA), boasting an IC 50 of 0.33 nM, and demonstrates approximately 1700-fold selectivity for AURKA over AURKB. It induces cell cycle arrest and apoptosis, making it a valuable compound for cancer research [1].

RIPK-IN-4 is a potent, selective RIPK2 inhibitor with nanomolar activity and oral bioavailability for studying innate immune pathways.

Atiprimod: an oral azaspirane inhibiting STAT3, blocking IL-6/VEGF pathways, and promoting apoptosis by downregulating Bcl-2 and Mcl-1.

Colletofragarone A2 from Colletotrichum sp. blocks mutant p53 and HSP90, aiding cancer treatment.

Potent EGFR blocker; acts on WT, L858R/T790M (IC50: 1.7 nM), less on T790M/C797S; stalls cell cycle, induces apoptosis, deters metastasis.

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.

Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.

Necrocide 1 is a inducer of cancer cell necrosis that is not inhibited by caspase, BCL2 , or TNFα, and acts through the mitochondrial regulatory pathway.

Thaspine: inhibits topoisomerase IB, reduces VEGF, stops endothelial cell growth via PI3K/MAPK pathways.

RET-IN-24 (Compound 26) is a selective inhibitor of RET tyrosine kinase, demonstrating antitumor activity [1].

TNIK-IN-6 (Compound 9) acts as an inhibitor of Traf2 and Nck-interacting kinase (TNIK), exhibiting an inhibitory concentration (IC50) of 0.93 μM, a kinase

CR6086: potent EP4 antagonist with DMARD effects, low Ki (16.6 nM), and specific anti-inflammatory action.

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

PBI-1393 can be used as an enhancer for Th1 type cytokine production and primary T cell activation.

Ac-YVAD-pNA, a specific substrate for Caspase-1, serves to detect Caspase-1 activity, a crucial mediator of inflammatory processes [1] [2].

MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor.

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM.

Z-LLY-FMK (Calpain Inhibitor IV) serves as an inhibitor of calpain, a family of proteases implicated in the apoptosis of various cell systems.

GSK2245035: selective nasal TLR7 agonist, boosts Type-1 IFN (pEC50: 9.3 IFNα, 6.5 TFNα), curbs Th2 cytokines in blood cultures.

MRT199665, a selective MARK/SIK/AMPK inhibitor, blocks SIK CRTC3 S370 phosphorylation and triggers apoptosis in AML cells.

A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].

CIL62 is a caspase-3/7-independent inducer of cell death. The mechanism of action of CIL62 is Necrostatin-1 dependent cell death [1].

Ac-YVAD-AOM is a selective and potent caspase-1 inhibitor showing antitumor activity and potential analgesic activity.

SAFit2 is a highly potent and selective inhibitor of fk506 binding protein 51 (FKBP51).Cost-effective and quality-assured

CDDO-2P-Im shows chemopreventive effect and reduces the size and severity of the lung tumors in the mouse lung cancer model.

ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar

Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.

VU0661013 is an effective and selective inhibitor of MCL-1.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma,

RH01386, a small molecule, prevents ER stress in β cells, inhibits proapoptotic genes, and may treat type 2 diabetes by restoring insulin secretion.

Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor.

M3541: an oral ATM inhibitor with antitumor effects, hinders DNA repair and promotes cancer cell death.

GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.

MC4033 exhibits inhibitory concentration 50 (IC50) values of 39.4 µM in HCT116, 52.1 µM in H1299, 41 µM in A549, and 30.1 µM in U937 [1].

DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values ​​of 10 nM and 800 nM for human COX-2 and COX-1.Cost-effective and quality-assured.

PP5-IN-1 is a serine/threonine protein phosphatase-5 (PP5) inhibitor with potential anticancer activity that induces apoptosis in cancer cells.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).

PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has anti-tumor activity and induces apoptosis.

PD-L1-IN-3 is a PD-1/PD-L1 inhibitor for the study of tumors and immune diseases.

AZA197 (AZA-197) is a selective Cdc42 inhibitor.

Ac-DEVD-CHO is a specific Caspase-3 inhibitor (Ki: 230 pM).Ac-DEVD-CHO has an inhibitory effect in SLNT-induced apoptosis.

NSC-697923 inhibits UBE2N, triggers p53-dependent and JNK-mediated apoptosis, blocks DNA damage and NF-κB signaling in neuroblastoma cells.

Lartesertib (ATM Inhibitor-5) is an inhibitor of the serine/threonine protein kinase ATM with potential anticancer activity and can be used to study lung cancer

JHU395, an oral prodrug of glutamine antagonist DON, shows stable antitumor effects on MPNST in vitro and vivo.

Oditrasertib, a RIPK1 inhibitor characterized by an IC50 value below 100 nM, is employed in inflammation research.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.