Apoptosis

(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.

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

INU-152: pan-RAF inhibitor with potent anti-tumor effects on BRAFV600E cancers, inhibits MAPK in mutant cells, minimal side effects on RAS-mutant melanoma.

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

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

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

CPUY201112, a novel inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells.

Ataquimast is used in curing advanced receptor-positive breast cancer.

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

BPR1J-340, a novel potent FLT3 inhibitor, shows anticancer promise, with IC50 ~25 nM and GC50 ~5 nM, causing apoptosis in AML cells.

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

NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.

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

Ethylene glycol dimethacrylate, a methacrylate monomer, demonstrates cytotoxic and genotoxic impacts on human gingival fibroblasts (HGFs), elevating

YM281 is a potent EZH2 inhibitor, causes apoptosis and G0/G1 arrest, has antitumor activity in vivo, and may be researched for lymphoma.

Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures.

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

IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.

Caspase-3 activator 1 (compound 4b), a Ru(III) metal complex, effectively inhibits gastric tumor growth and metastasis by mediating caspase-3 cleavage.

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.

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

D359-0396 is an orally active NLRP3 inflammasome inhibitor that mitigates pyroptosis and reduces IL-1β release in macrophages by inhibiting the oligomerization

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.

HDAC1/CDK7-IN-1 (compound 8e) serves as a dual inhibitor targeting both CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM , respectively.

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

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].

2-O-methyl PAF C-16 is a synthetic analog of platelet-activating factor (PAF) featuring a methyl group attached via an ether linkage at the sn-2 position. While the specific biological activities of 2-O-methyl PAF C-16 remain undercharacterized, studies with its C-18 counterpart have demonstrated its ability to modulate various biological processes. These processes include reducing plasma membrane fluidity and hindering the invasiveness of tumor cells in embryonic chick hearts. Furthermore, in rat astrocytes, the C-18 analog prompts the release of significant amounts of nitric oxide (NO) through a mechanism that involves the activation of nitric oxide synthase (NOS).

iMAC2 hydrochloride, a potent inhibitor of the mitochondrial apoptosis-induced channel (MAC), demonstrates an IC50 of 28 nM and an LD50 of 15000 nM. It exhibits an anti-apoptotic effect by blocking the release of cytochrome c [1].

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].

(+)-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).

C 87: Small-molecule TNF-α inhibitor, binds TNFα, inhibits cytotoxicity with IC50 of 8.73 μM, blocks signaling.

SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.

10-OAHSA is a newly discovered endogenous lipid categorized within the group of branched fatty acid esters of hydroxy fatty acids (FAHFAs). This specific FAHFA comprises oleic acid esterified to 10-hydroxy stearic acid. It stands out among its FAHFA counterparts for its potential bioactive properties, similar to other members of its family such as PAHSAs, which are notably prevalent in the adipose tissue of AG4OX mice exhibiting glucose tolerance due to overexpression of the Glut4 glucose transporter specifically in adipose tissue. Like other FAHFAs, 10-OAHSA may play significant roles in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, which suggests its importance in managing metabolic syndrome and inflammation.

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

GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.

SF5 is an inhibitor of the apoptosis pathway through JNK-p53-caspase apoptotic cascade.

NWP-0476 is a modified BCL-2/BCL-xL inhibitor with enhanced specificity for BCL-xL, suitable for research on relapsed T-acute lymphoblastic leukemia (T-ALL) [1

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

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

Vatalanib hydrochloride (PTK787 hydrochloride) is a VEGF inhibitor that reduces the number and area of Aβ plaques in the cortex of 5xFAD mice.

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.

EP1013 is a broad-spectrum selective inhibitor of Caspase used in the study of type 1 diabetes.

BAI1 hydrochloride is a selective inhibitor of the apoptosis factor BAX, functioning through an allosteric mechanism. By binding to BAX, it allosterically inhibits its activation, showcasing potential applications in the research of diseases mediated by BAX-dependent cell death [1].

APE1-IN-2 (AP1), a Pt(IV) proagent, targets APE1 protein, induces DNA damage, and triggers apoptosis with anticancer effects.

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

C6 urea ceramide blocks neutral ceramidase, boosts ceramide levels, halts HT-29 cancer cell growth, and shrinks HT-29 tumors in mice when dosed.

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

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

RIP1 Kinase Inhibitor 8 (Compound 77), a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor, exhibits an IC50 of 20 nM and effectively

CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.

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.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively.

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM).

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

AM-8735 is an inhibitor of MDM2 ( IC50: 25 nM).

M109S is a novel small molecule that shields cells from mitochondria-dependent apoptosis, demonstrating effectiveness both in vitro and in vivo.

PD-1/PD-L1-IN-33 (Compound N11), a PD-1/PD-L1 inhibitor, effectively impedes the interaction between PD-1 and PD-L1 with an IC50 of 6.3 nM.

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.

LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.

NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].

c-Met/HDAC-IN-3: dual inhibitor; IC50: c-Met 12.5 nM, HDAC1 26.97 nM; induces apoptosis, G2/M arrest.

"DC_AC50 inhibits Atox1/CCS to reduce cancer cell growth and prevent chemotherapy resistance."

USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).

TBTDC serves as a multifunctional organic photosensitizer exhibiting aggregation-induced emission characteristics, optimal for in vivo bioimaging and

CUR61414 is a cell-permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM) and selectively binds to smoothened (Ki = 44 nM).

BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].

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

HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage,

Ezatiostat HCl (TLK199) inhibits glutathione S-transferase, GSTP1-1 specifically, and may treat cytopenias.

Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.

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

SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.

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.

eIF4A3-IN-18, a silvestrol analogue with EC50s: 0.8/35/2 nM, inhibits eIF4F complex and is cytotoxic (LC50: 0.06 nM) for cancer research.

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

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

PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM.

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

Erythro-Austrobailignan-6: orally active, anti-cancer, inhibits DNA topoisomerases, induces apoptosis, boosts p38/JNK phosphorylation.

Ponicidin, a diterpenoid from Rabdosia rubescens, has immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer properties.

Bcl-2-IN-12 (Compound 1) is a potent Bcl-2 inhibitor with an IC50 value of 6 nM, utilized in cancer research [1].

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

CPT-Se3, a camptothecin derivative, boosts anticancer activity, triggers apoptosis in Hep G2, and is cytotoxic to various cells with IC50 of 2.19-4.7 μM.

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

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].

Vepafestinib is a RET inhibitor with potential antineoplastic activity[1].

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

BAX-IN-1 is a potential selective inhibitor of Bcl-2-associated X protein (BAX).

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