Apoptosis

HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.

LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.

FD2157, a photosensitive PI3K inhibitor, exhibits inhibitory IC50 values of 43 nM for PI3Kα, 83 nM for PI3Kβ, 84 nM for PI3Kγ, and 14 nM for PI3Kδ.

Anticancer Agent 153 (Compound 3) promotes apoptosis through the generation of Reactive Oxygen Species (ROS) and elevates the loss of Mitochondrial Membrane

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer.

Thalidomide-PEG4-NH2 HCl, a cereblon ligand-linker for PROTAC.

KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.

Thalidomide-derived cereblon ligand with PROTAC linker as an E3 ligase ligand-linker conjugate, in hydrochloride form.

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4

Apoptosis Inducer 11 (compound 3u) promotes apoptosis via the mitochondrial pathway and elicits a G2/M block alongside a marked reduction in the S phase within

Onercept, a recombinant soluble form of the human tumor necrosis factor-alpha (TNF-α) p55 receptor, is utilized in the study of Crohn's disease [1].

Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.

Dimethachlor is a pesticide and herbicide used in wetland areas.

Topo I/II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K/Akt/mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

2'-Epi-2'-O-Acetylthevetin B (GHSC-74), a cardiac glycoside extractable from Cerbera manghas L.

Anti-MousePD-1(LALA-PG) Antibody (RMP1-14) is an IgG2a, κ antibody inhibitor derived from mice that targets and inhibits mouse PD-1.

Ac-LEHD-AMC, a fluorogenic caspase-9 substrate, releases fluorescent AMC upon cleavage, aiding caspase-9 activity measurement.

Ferroptosis-IN-1, a diterpene derived from A.

AChE-IN-81 (compound 22) is a reversible, selective inhibitor of AChE with an 80.0% inhibition rate and an IC50 of 3.7 μM. It binds to AChE with an affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces apoptosis in zebrafish brain cells and shows potential neuroprotective activity in an H2O2-induced SH-SY5Y cell damage model.

Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].

Caerin 1.1 TFA, a host defense peptide derived from the Australian tree frog Litoria's glandular secretions, exhibits anti-proliferative effects on HeLa cells

Ferroptosis-IN-3 (Compound 25), a ferroptosis inhibitor, demonstrates potent activity by inhibiting RSL3-induced ferroptosis in HT-1080 cells (EC50: 8.6 nM).

QN523 has drug-like traits, kills cancer cells in vitro, effective in vivo against pancreatic cancer, works via autophagy.

Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM), exhibits an IC50 value of 3.38 μM against human dermal fibroblasts (HDF) and

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.

BRD4 Inhibitor-39 (compound 12m) is an orally active inhibitor of BRD4 with an IC50 of 0.02 μM. It can induce apoptosis and demonstrates antitumor activity.

Ara-SH, a derivative of Cytarabine with a mercaptopropionic acid substitution, serves as the initiator for the self-assembly of a smart, co-loaded Cytarabine

BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].

12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.

PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.

Antiproliferative Agent-27 (Compound 11) is a notable antiproliferative agent that markedly diminishes tumor cell colony formation and induces apoptosis,

PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.

Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.

N-Stearoyltyrosine (N-(1-Oxooctadecyl)-L-tyrosine) is an analog of Anandamide. It exhibits neuroprotective effects by safeguarding the CA1 region of the hippocampus in a gerbil ischemia-reperfusion model. Additionally, N-Stearoyltyrosine inhibits free radical generation, enhances antioxidant capacity, and reduces IR-induced apoptosis (cell apoptosis).

CWI1-2 HCL: Potent IGF2BP2 inhibitor, induces apoptosis/differentiation, targets leukemia therapy.

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

SBP-0636457: SMAC mimetic, IAP inhibitor, binds BIR-domains (Ki=0.27μM), potential in tumor/cancer research.

BM-962 (Compound 31) is a potent small-molecule inhibitor with an IC50 value of 4 nM (Ki=0.8 nM) for Bcl-2 and an IC50 of 3.9 nM (Ki<1 nM) for Bcl-xL. It inhibits H1417 and H146 cell lines with IC50 values of 9 and 13 nM, respectively, and shows potential for use in cancer research.

DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.

Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.

DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.

Didocosahexaenoin, omega-3 diglyceride, disrupts mitochondria, induces ROS, apoptosis, and is cytotoxic to prostate cancer cells.

Thalidomide-4-C3-NH2 HCl is a cereblon ligand for CRBN recruitment, used to make PROTACs with a linker.

Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.

STM3006 is an orally active, selective and and potent METTL3 inhibitor with antitumor activity for the study of acute myeloid leukemia (AML).

SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 / DHCR24 / ROS axis and driving apoptosis in

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in

BM-1197, a highly potent and specific dual inhibitor of Bcl-2 and Bcl-xL, effectively targets these proteins with IC50 values of 3.5 nM and 5.2 nM for Bcl-2 and

ReACp53 inhibits amyloid formation, restores p53 in cancer cells and HGSOC-derived organoids.

FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.

XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.

Anticanceragent 268 (Compound 4k) is a potential antitumor agent. It exhibits antiproliferative effects on HepG2 cells, with an IC50 value of 6.08 μM. Additionally, Anticanceragent 268 induces apoptosis and inhibits colony formation and migration of HepG2 cells.

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

RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.

PZ703b TFA, a Bcl-xl PROTAC degradation agent, promotes apoptosis and halts bladder cancer cell proliferation, making it a pertinent investigative compound for

Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.

TRP-601 is a caspase inhibitor.

Compound 106 (compound 10ic) induces apoptosis in B16-F10 melanoma cells and potently inhibits metastatic nodules in mouse models of lung metastatic melanoma,

Thalidomide-PEG3-NH2: a cereblon-based E3 ligase ligand-linker for PROTAC tech.

IPH10 is an anticancer agent with strong antitumor effects in vivo and exhibits no liver or kidney toxicity. It significantly increases the reactive oxygen species (ROS) levels in tumor cells, decreases mitochondrial membrane potential, and induces apoptosis (apoptosis) in these cells.

SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.

AM-8553 is potent and selective piperidine the MDM2-p53 interaction inhibitor.

Glutathione arsenoxide hydrochloride: anti-cancer, inhibits tumour metabolism, targets ANT, promotes apoptosis, marks cell proteins.

Fludarabine triphosphate (F-ara-ATP) trisodium inhibits DNA synthesis; IC50 2.3 μM, Ki 6.1 μM, blocks DNA primase, prompts apoptosis.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

Thalidomide-based cereblon ligand with 2-unit PEG linker for PROTAC, in hydrochloride form.

Voreloxin (SNS-595) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

PERK-IN-4 is a potent and selective PERK inhibitor with an IC50 value of 0.3 nM.PERK-IN-4 can be used in the study of cancer and neurological disorders.

eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.

Tasisulam triggers apoptosis, halts mitosis, and normalizes blood vessels to combat cancer.

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

KP1019 is now discontinued.

PTD-p65-P1: a NF-kappaB inhibitor blocking activation from multiple inflammatory stimuli.

RIPK2-IN-2, a RIP2 kinase PROTAC inhibitor, blocks proinflammatory signaling in autoinflammatory diseases.

Anticanceragent 273 (Compound 9q) is an effective anticancer compound identified from matrine. It inhibits cancer cell proliferation, with an IC50 of 4.48 μM against HeLa cells. Anticanceragent 273 exerts its anticancer effects by modulating PI3K/AKT expression and activating activating transcription factor 4 (ATF4), which induces endoplasmic reticulum stress and triggers apoptosis. It holds potential for cancer research, including cervical cancer.

TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.

Cereblon ligand for PROTAC R&D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.

KT5823 is a cGMP-dependent protein kinase (PKG) inhibitor that increases iodide ion uptake by regulating the expression of sodium iodide symporter protein.

eIF4A3-IN-7: Potent eIF4A3 inhibitor, potential cancer/dysproliferation research (WO2019161345A1, Compound 8).

PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.

D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1/Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.

F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.

FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice.FC-116 induces apoptosis and promotes protein degradation.

MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, demonstrating dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX.

GPX4-IN-6 is a GPX4 inhibitor with antitumor activity.GPX4-IN-6 induces iron death and is used for the treatment and prevention of triple-negative breast cancer

HSP90-IN-18 inhibits Hsp90 with 0.39 μM IC50, useful for viral, neurodegenerative, and inflammatory research.

SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells.

Met-12 is a peptide inhibitor of the Fas receptor. It suppresses Fas receptor-mediated apoptosis in photoreceptor cells and reduces Caspase activation, making it a potential candidate for research on photoreceptor protectants.

CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.

Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.

MDM2/4-p53-IN-2 (2q) is a dual MDM2/MDM4 inhibitor, p53 activator; IC50: 70.7 nM(MDM2), 81.4 nM(MDM4); tumor suppressor.

H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.