Apoptose

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

Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on

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

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

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

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

ERα antagonist 1 is a selective, potent, covalent estrogen receptor alpha (ERα) antagonist that blocks the cell cycle of MCF-7 cells in G0/G1 phase and induces

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.

SD 1008 is a JAK2/STAT3 signaling pathway inhibitor. SD 1008 inhibits activation of STAT3, JAK2, and Src.

RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their

WF-210 is an effective activator of procaspase-3 that acts by inducing apoptosis in cancer cells and reducing tumor growth.

Necrostatin-1 (Nec-1) (inactive control), an inactive analog of Necrostatin-1, functions as a potent inhibitor of necroptosis [1].

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].

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

PLK1/BRD4-IN-1 (9b) is an orally active dual inhibitor of PLK1 (IC50: 22 nM) and BRD4 (IC50: 109 nM).

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

eIF4A3-IN-9, a silvestrol analogue, disrupts eIF4F complex assembly; EC50s: 29/450/80 nM (myc/tub-LUC, MB-231 cells); for cancer research.

SM-433: Smac mimetic, blocks IAPs, strong XIAP BIR3 affinity (IC50 <1 μM). See patent WO2008128171A2.

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

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

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

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].

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

WEHI-345 analog is an Src inhibitor.

TMX-2164: strong, irreversible BCL6 inhibitor, IC50=152 nM, long-lasting action, inhibits cell proliferation.

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

ER Proteostasis Regulator-1 (Compound 481) is a potent modulator of endoplasmic reticulum proteostasis with research applications in Alzheimer's disease and

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

Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68, exhibiting an EC50 of 170 nM.it is utilized in the study of autoimmune chronic inflammatory diseases [1

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.

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.

MTI-31 (LXI-15029) is a potent oral mTORC1/2 inhibitor with a Kd of 0.20 nM, >5,000-fold selectivity, and an IC50 of 39 nM.

Ethylene dimethanesulfonate has selective pro-apoptotic effects on LCs. Ethylene dimethanesulfonate is a mild alkylating, non-volatile methanesulfonic diester

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

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

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

(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.

GW405833 hydrochloride, a potent and selective agonist of the cannabinoid-2 (CB2) receptor (EC 50 = 0.65 nM; maximum inhibition = 44.6%), exhibits significant antihyperalgesic effects in various rodent pain models [1] [2] [3].

BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.

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.

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

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

PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) effectively inhibits the PD-1/PD-L1 interaction (IC 50 = 0.029 μM) and demonstrates selective binding affinity to PD-L1

UNC3474, a small molecule ligand, selectively interacts with the aromatic methyl-lysine binding cage of the tumor protein 53BP1 Tudor domain (TT), exhibiting a

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

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

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

Antitumor agent-60 inhibits growth by targeting RAS-RAF, binding CRAF (Kd: 721.3 nM), boosting p53/ROS, causing apoptosis, and arresting G2/M phase.

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

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.

MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1,

HAPSBC, an S-benzyl iron chelator, modulates the intracellular distribution of ^59Fe [1].

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

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

Lacutoclax (LP-108) is an orally active and selective Bcl-2 inhibitor with antitumor activity both in vivo and ex vivo，lymphoma and leukemia.

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

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).

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

ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.

Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].

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

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

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

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

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.

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

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.

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

Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.

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

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].

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.

FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.

GSK-2245035 maleate is a selective Toll-like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties.

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

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

PK68 selectively inhibits RIPK1 (IC50=90nM), potentially useful in inflammation and cancer metastasis studies.

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.

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

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

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].

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

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

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].

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).