Apoptosi

CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).

Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.

Varlilumab (CDX-1127) is a novel human IgG1 anti-CD27 monoclonal antibody. Varlilumab has antitumor activity and can be used to study advanced solid tumors.

ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.

Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.

Albanol B, from mulberries, combats Alzheimer's, bacteria, and oxidation, hinders cancer growth, and triggers cell arrest and apoptosis.

YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.

RTX-002 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. This compound is applicable in the research of autoimmune diseases such as systemic lupus erythematosus and multiple sclerosis.

PL120131 is a PD-1/PD-L1 inhibitory peptide that disrupts the interaction between PD-1 and PD-L1 by binding to PD-1. This compound can inhibit the apoptosis signaling pathway mediated by PD-1, thereby preventing apoptosis (apoptosis) in Jurkat cells and primary lymphocytes. Additionally, PL120131 supports cytotoxic T lymphocytes (CTL) in exhibiting antitumor activity.

A unique collection of 1760 apoptosis-related compounds for apoptosis research, research in tumorigenesis, and anti-cancer drug screening;

Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.

Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in

Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.

TNF-α (31-45), human is a peptide of tumor necrosis factor-α.

CS4 is a selective HDAC inhibitor, with IC50 values for HDAC1, HDAC6, HDAC8, HDAC4, and HDAC11 reported as 38 nM, 12 nM, 5.8 μM, 19 μM, and 61 μM, respectively. It enhances the acetylation of α-tubulin and histone 3 (histone 3). Additionally, CS4 activates PPARγ and blocks glycolysis (glycolysis). It induces cell cycle arrest at the G2 phase and triggers apoptosis (apoptosis), exhibiting anticancer effects both in vitro and in vivo.

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density

A unique collection of 193 endoplasmic reticulum stress (ER stress) related compounds used for high throughput screening (HTS) and high content screening (HCS);

PROTACKDM4 degrader-1 (Compound 11) is a proteolysis-targeting chimera (PROTAC) degrader specifically designed for KDM4. It effectively degrades KDM4A-C while sparing KDM4D. In esophageal cancer cells, PROTACKDM4 degrader-1 demonstrates strong antiproliferative activity, inducing apoptosis and cell cycle arrest, and inhibits lysine demethylation of histone H3.

1,2,3,4-Tetrahydronaphthalen-2-ol exhibits weak inhibitory activity against Bcl-xL and is widely used in biochemical experiments and drug synthesis research.

PH14, a dual PI3K/HDAC inhibitor, demonstrates potent inhibition with IC50 values of 20.3 nM for PI3Kα and 24.5 nM for HDAC3.

KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (>10 μM); human ABHD16A IC50: 90±20 nM.

Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including

Thalidomide-based cereblon ligand linked to PROTAC technology as E3 ligase ligand-linker.

P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).

S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is effective against BCL-2 mutations, including G101V and D103Y.

Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells

Bim BH3 is a bioactive peptide that belongs to the pro-apoptotic Bcl-2 family of proteins.

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

PRMT5-IN-31 (Compound 3m), a selective PRMT5 inhibitor (IC50: 0.31 μM), increases hnRNP E1 protein levels by occupying the substrate site of PRMT5 and

RMC-9805(Zoldonrasib) is a KRAS G12D inhibitor with anti-tumor and anti-proliferative activity for the study of pancreatic cancer.

MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.

FR900359 is a macrocyclic Gq protein inhibitor that inhibits melanoma cell proliferation and can be used to study asthma, inflammation and cancer.

Pimagedine is a prototype therapeutic agent for the prevention of formation of advanced glycation endproducts.

Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.

Sterigmatocystine, a G1 phase and DNA synthesis inhibitor, curbs p21 and is a mycotoxin precursor from Aspergillus versicolor.

Disitertide (P144) is an inhibitor of TGF-β1.

Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.

YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.

PROTACGPX4 degrader-4 is a GPX4 PROTAC degrader with a DC50 of 5.32 nM. It inhibits the activity of cancer cell lines RT4, T24, and J82 with IC50 values of 0.09, 2.97, and 7.58 μM, respectively. This compound elevates lipid ROS levels and induces ferroptosis in T24 and RT4 cells. In T24 tumor-bearing BALB/c nude mouse models, PROTACGPX4 degrader-4 demonstrates antitumor activity. It is applicable to bladder cancer research.

"(±)-Enterodiol, the racemate of Enterodiol, is metabolized from lignans found in whole-grain cereals, nuts, legumes, flaxseed, and vegetables by human intestinal bacteria. This compound exhibits apoptotic effects in colorectal cancer (CRC) cells and has been identified to possess anti-cancer activities [1] [2]."

RMC-6291: Oral, covalent KRAS G12C inhibitor, blocks signaling, forms tri-complex with CypA, suppresses RAS activity in tumors.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

PROTAC Bcl-xL degrader-2, based on von Hippel-Lindau ligand, is a potent degrader of Bcl-xL (a Bcl-2 family member), demonstrating an IC 50 of 0.6 nM.

NEP162 is a BRD4 PROTAC degrader with DC50 values of 1.2 μM in SW480 cells and 1.6 μM in U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibiting tumor growth and inducing apoptosis. It is applicable in research on cancers such as osteosarcoma, colorectal cancer, and non-small cell lung cancer.

Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.

Akt/NF-κB/MAPK-IN-1 (compound 2m) serves as a potent, orally active inhibitor targeting NO with an IC50 of 7.70 μM and demonstrates low toxicity.

HDAC6-IN-22 (compound 30), an HDAC6 inhibitor, exhibits an IC50 of 4.63 nM and demonstrates antiproliferative effects against multiple myeloma both in vitro and

Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate

GR-1405 is a human monoclonal antibody (mAb) that targets B7-H1/PD-L1/CD274. It enhances the antitumor immune response mediated by cytotoxic T lymphocytes (CTL) against tumor cells expressing PD-L1. GR-1405 is applicable in research related to lymphomas and solid tumors.

Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].

PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.

RIPK1-IN-17 is a dual inhibitor of RIPK1 and RIPK3 inhibits necrosis by inhibiting phosphorylation of RIPK1, RIPK3 and MLKL,in a tnf-induced inflammation model.

Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.

7-Methoxy-1-tetralone may have insecticidal activity.

Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.

MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080

L-threo-PPMP blocks GlcT, curbs glycosphingolipid creation, and triggers cell death, showing anti-cancer effects.

XZ739: Cereblon-based PROTAC, degrades BCL-XL (DC50 2.5 nM in MOLT-4, 16hr), induces caspase apoptosis.

2,2'-Dihydroxy chalcone inhibits β-glucuronidase (IC50=1.6 μM) and lysozyme (IC50=1.4 μM), and fights E. coli, S. fowleri, S. albicans, S. aureus.

Pyridinium bisretinoid A2E (A2E) is a fluorescent molecule isolated from the lipofuscin of retinal pigment epithelium, a weak photosensitizer.

HDAC-IN-84 (compound 4a) is a potent HDAC inhibitor with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8, and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC11, respectively. It effectively inhibits the proliferation of leukemia cells without causing toxicity.

IDH1/2-IN-1 (Compound 6b) is a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. This compound effectively inhibits tumor growth by suppressing tumor cell proliferation and activating antioxidative enzymes to enhance host defense. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating significant anti-tumor activity. It is also utilized in leukemia research.

Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.

Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.

NA-Ir is a ferroptosis (Ferroptosis) inducer that targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to stimulate ferritin autophagy (). It also induces the production of reactive oxygen species (ROS) through photodynamic therapy (PDT), depletes glutathione (GSH), and downregulates glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and ferroptosis. NA-Ir exhibits enhanced anticancer activity under light exposure and selectively inhibits cancer cells with high H2S content.

Sanggenon G inhibits XIAP by binding its BIR3 domain; affinity is 34.26 μM, boosting caspase activation.

Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .

AS-99 TFA: potent ASH1L inhibitor, IC50=0.79 μM, combats leukemia, inhibits cell growth, induces apoptosis.

Pantinin-1 is an antimicrobial peptide found in the venom of the emperor scorpion (Pandinus imperator). This compound exhibits strong antibacterial activity against Gram-positive bacteria and fungi, but has weaker effects on Gram-negative bacteria. Additionally, Pantinin-1 demonstrates very low hemolytic activity on human red blood cells and possesses anticancer properties, specifically inducing apoptosis in tumor cells.

HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

Epoprostenol sodium (Prostaglandin I2 sodium salt) is a vasodilator and a synthetic prostacyclin that can be used to study pulmonary hypertension.

Aloeresin G, a chromone glycoside isolated from Aloe, exhibits a moderate inhibitory effect on TNFα-induced NF-κB transcriptional activity, evidenced by an IC50

QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.

Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

Targaprimir-96 is a potent microRNA-96 (miR-96) processing inhibitor.

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.

Ac-FEID-CMK: Potent inhibitor for zebrafish GSDMEb, reduces pyroptosis, and lessens septic AKI.

ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to

Trichostatin C, a natural glycosylated hydroxamate, is a histone deacetylase inhibitor with antifungal properties and can induce cell differentiation.

Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.

[1,1'-Biphenyl]-3-amine is an inhibitor of MAO-A and MAO-B and can inhibit the cell viability of HT-29, HEK 293, and MCF-7 cells.

ZYH-23 is a potent inhibitor of necroptosis. It targets HSP90 to inhibit the phosphorylation of RIPK1, RIPK3, and MLKL, effectively blocking programmed cell necrosis.

UNC10245380 is a CIB1 inhibitor with an IC50 of 8 μM. It also inhibits the phosphorylation of AKT and ERK while upregulating the expression of TRAIL-R1/D5. UNC10245380 specifically kills cancer cells that are dependent on CIB1, demonstrating its potential value in the development of CIB1 probes and cancer research.

PD1-PDL1-IN 1 TFA (compound 16) is a potent inhibitor of programmed cell death 1 (PD-1), functioning as an immune modulator [1].

TMX1 is a molecular glue degrader targeting BRD4, selectively recruiting the ubiquitin ligase CUL4-DCAF16 complex to BRD4 (BD2.

β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer employed in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-

Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).

Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.

Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].

Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin > R837 [1].

PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.

A947 is a potent and selective SMARCA2 PROTAC that induces the degradation of SMARCA2, with significant antitumor activity in SMARCA4-mutant NSCLC cells.

ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP.

Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].