Apoptosis

AT-9283 L-lactate is an inhibitor of aurora kinase.

BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM).

Sirt1/2-IN-2 (compound hsa55) serves as a dual inhibitor for SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM, respectively.

SAFit1 is an inhibitor of FK506 binding protein 51 (FKBP51)-specific (Ki: 4±0.3 nM).

MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein

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.

Riboxin (IDP), an orally administered purine derivative known as hypoxanthine riboside, exhibits antihypoxic and antihyperthermic effects.

BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.

Myrothecine A, a trichothecene mycotoxin discovered in M. roridum, exhibits anticancer properties. It effectively inhibits the proliferation of various cancer cell lines, specifically A549, MCF-7, HepG2, and SMMC-7721, with IC50 values of 95, 70, 60, and 25 µM, respectively. At a concentration of 50 µM, Myrothecine A induces G1 cell cycle arrest in HepG2 cells and promotes apoptosis in SMMC-7721 cells by elevating levels of Bax and cleaved caspase-3, -5, and -8.

FOXO1-IN-3 is a highly-selective, orally active inhibitor of FOXO1 that diminishes hepatic glucose production and enhances insulin sensitivity and glucose

PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM).

IM156, a Metformin derivative, activates AMPK, enhances cognition in aging animals, and inhibits OXPHOS in solid tumor research.

INI-43 targets Kpnβ1, disrupting nuclear transport in cervical/esophageal cancers, affecting NFAT, NFκB, AP-1, NF localization.

Artonin E, a prenylated flavonoid, induces apoptosis and S-phase arrest, disrupting the mitochondrial pathway for cancer research.

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

HA-14-1, a small molecule, binds the surface pocket of Bcl-2 proteins (IC50= ~ 9 µM), including Bcl-xl and Bcl-W, and disrupts their interaction with the Bak peptide. This action induces apoptosis by activating Apaf-1 and caspase-9 and -3. Additionally, HA-14-1 effectively induces apoptosis in human acute myeloid leukemia (HL-60) cells, with a 50 µM concentration resulting in a 90% loss of cell viability.

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

Sphingosine-1-phosphate (S1P), a bioactive lipid crucial in numerous signaling pathways, undergoes irreversible degradation by membrane-bound S1P lyase, producing (E)-2-Hexadecenal, a derivative of sphingolipid breakdown. This compound can be oxidized to (2E)-hexadecenoic acid by long-chain fatty aldehyde dehydrogenase before being activated through linkage to coenzyme A. Notably, (E)-2-Hexadecenal induces cytoskeletal reorganization, leading to cell rounding, detachment, activation of JNK pathway targets, and ultimate apoptosis in a variety of cell types. Furthermore, it readily forms aldehyde-derived DNA adducts through reactions with deoxyguanosine and DNA.

Ro 41-5253 is a RARα antagonist with antitumor activity that inhibits the proliferation of ZR-75.1 estrogen receptor-positive breast cancer cells.

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.

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

AGN194204 (IRX4204), an oral RXR agonist, inactive against RAR, has Kd 0.4-3.8 nM & EC50 0.08-0.8 nM, with anti-inflammatory and anticarcinogenic properties.

4E2RCat is an inhibitor of eIF4E-eIF4G interaction (IC50 = 13.5 μM) and is capable of blocking coronavirus replication as monitored by viral protein expression

PD-1/PD-L1-IN-27: potent anti-cancer, IC50 134nM, minimal T cell harm, boosts CD8+ T cells, reduces fatigue.

YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (

Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).

Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl

INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.

Famitinib malate (SHR1020) is a potent oral kinase inhibitor targeting c-kit, VEGFR-2, and PDGFRβ, with IC50s 2.3, 4.7, 6.6 nM, useful for cancer research.

Pelcitoclax (APG-1252) is a powerful inhibitor of the Bcl-2 and Bcl-xl proteins, displaying significant antineoplastic and pro-apoptotic properties[1].

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

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.

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

TL02-59: Fgr inhibitor (IC50=0.03nM), also targets Lyn (0.1nM), Hck (160nM), halts acute myelogenous leukemia growth.

BTM-3528 is a mitochondrial protease OMA1 activator that induces an overactivation of the mitochondrial integrated stress response (ISR).

ASC-69 (APY69) is a promising potent inhibitor of the PD-1/PD-L1 signaling pathway, classified as a small-molecule compound [1].

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.

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

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

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.

ICy-Q, a NIR reagent activated by NQO-1, triggers pyroptosis in pancreatic cancer cells, aiding diagnosis.

M867 is a selective, reversible caspase-3 inhibitor, possessing an IC50 of 1.4 nM and a Ki value of 0.7 nM, demonstrating anti-apoptotic activity [1].

Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively.

WNY1613: Potent PI3Kδ inhibitor with anti-NHL properties, induces apoptosis in cells, affects phosphorylation in vitro/in vivo.

E235, an activator of the transcription factor 4 (ATF4), enhances the integrated stress response (ISR) and DNA damage response, thereby reducing cell viability

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds the RIP3 kinase domain (IC50: 0.9 nM), and inhibits kinase

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

WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.

AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.

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].

Purinostat mesylate, a selective HDAC inhibitor (IC50: 0.81-11.5 nM), induces apoptosis and has potent anti-leukemic effects.

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage.

PIM447 (LGH447) is a pan-PIM kinase inhibitor with anti-tumor and bone protective effects. PIM447 reduces the viability, and motility of HuH6 cell.

AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.

13h (hGGPPS-IN-3), a strong C2-ThP-BPs hGGPPS blocker, triggers MM cell apoptosis and shows in vivo anti-myeloma effects.

Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability.

TM5441, an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 values ranging from 13.9 to 51.1 μM, effectively induces intrinsic apoptosis across multiple human cancer cell lines. Additionally, it mitigates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] [2].

RET-IN-17 inhibits RET kinase; may help in IBS pain and RET-activated cancers.

Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.

KRIBB3: novel anticancer microtubule inhibitor; halts MDA-MB-231 cell migration/invasion by targeting Hsp27 phosphorylation.

Cerivastatin is an HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects and can be used to study primary hyperlipidemia.

Eeyarestatin I blocks ER protein degradation, hinders p97/atx3 processes, and induces anticancer proteins.

NSC 48160 is an anti-pancreatic cancersmall molecule that inhibits growth and enhance apoptosis of pancreatic cancer cells through the mitochondrial pathway.

Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.

Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.

Potent γ-secretase inhibitor; IC50: 1.2 nM (cell), 6.2 nM (cell-free); lowers Aβ in mice/guinea pigs' brain, CSF, plasma.

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.

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

SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.

BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].

Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].

Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].

Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects,

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

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

Anticancer agent 105, a thienopyrimidine scaffold-based compound, exhibits selective toxicity towards melanoma and induces apoptosis.

Anticancer agent 127 (142D6), an IAP inhibitor, covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, with IC50 values of 12 nM, 14 nM, and 9 nM,

RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting

ST1074, a dual inhibitor of CerS2 and CerS4, promotes apoptosis and is applicable in cancer research [1].

BQZ-485, a potent GDI2 inhibitor, interacts with Tyr245 to disrupt the native GDI2-Rab1A interaction.

Antitumor agent-97 (compound 42), an anticancer agent, effectively inhibits proliferation and autophagy in MGC 803 cells, induces apoptosis, and enhances ROS

PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.

CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.