YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agentIC50 value:Target: MDM2/p53YH239-EE inhibits the growth of OCI-AML-3 cells with wild type p53 by inhibiting the p53-MDM2 interaction. YH239-EE induces cell cycle arrest and causes potent cell apoptosis via activation of p53 and downstream targets in four AML cells (OCI-AML-3 and MOLM-13 with wt p53, NB4 with p53 mutation, and HL60 with p53 deletion).
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia[1].
Oblimersen is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen can be used for cancer research[1][2][3].
Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) prodrug with antitumor activity[1].
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage[1].
Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models[1].
MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy[1].
Bax inhibitor peptide V5 is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
5-Fluorouracil-13C4,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively.[1][2] Okadaic acid eliminate metazoan symbionts/parasites by apoptosis[3].
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis[1][2][3].
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway[1].
Benidipine is a potent and orally active calcium channel antagonist[1]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[2]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[3].
RIPK1-IN-8 (example 16), an aminoimidazopyridine, is a potent and selective RIPK1 inhibitor with an IC50 of 4 nM. RIPK1-IN-8 has the potential for inflammatory diseases research[1].
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2)[1].
Metronidazole hydrochloride (SC 326421) is an orally active nitroimidazole antibiotic, can be used to research anaerobic infections. Metronidazole hydrochloride can cross blood brain barrier and results inflammation and skeletal muscle contraction under long-term application[1][2][3][4].
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells[1].
Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM[1][2][3][4].
Antitumor agent-64 (Compound 8d) is a diosgenin derivative. Antitumor agent-64 exhibits potent cytotoxic activity against A549 cell line. Antitumor agent-64 induces A549 cells apoptosis via the mitochondria-related pathway[1].
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research[1].
Beta-zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells[1]. Beta-zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid[2].
Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan is used for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
SM-1295 is a potent, selective cIAP1 and cIAP2 inhibitor with Ki of <10 nM, displays >900-fold for cIAP1 over XIAP; potently inhibits cell growth in the MDA-MB-231 and SK-OV-3 cancer cell lines and induces apoptosis at low nanomolar concentrations; efficiently induces degradation of cIAP1 protein in cancer cells, as well as cleavage of PARP, caspase-8, and caspase-3; induces cell death in a TNFα-dependent manner in both MDA-MB-231 and SK-OV-3 cancer cell lines.
A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3), shows micromolar potency toward Pim-1 and Pim-2 (Ki=1.5 and 17 uM); displays a high degree of selectivity for DAPKs and Pims against a panel of 468 kinases, with only two off-target interactions TYK2 and GAK; also displays no significant inhibition or activation of nicotinic, adrenergic, or muscarinic receptors at 10 uM; HS56 delayed force onset, decreased contractile force, and reduced LC20 phosphorylation in excised rat caudal arterial VSM tissues, lowers blood pressure in spontaneously hypertensive mice without affecting heart rate.
Verbenalin is Verbena glycoside, with anti-inflammatory, anti-fungal anti-virus activities. Verbenalin has a good effect on prostatitis. Verbenalin can reduce cerebral ischemia-reperfusion injury[1][2].
Cimiside E (25-Anhydrocimigenol xyloside) is a triterpene xyloside, Cimiside E possesses apoptotic action on gastric cancer cells, with an IC50 value of 14.58 μM. Cimiside E induces cell cycle arrest at G2/M phase, and mediates apoptosis through the induction of the Caspase cascade for both the extrinsic and intrinsic pathways[1][2].
S-Adenosyl-L-methionine (S-Adenosyl methionine) 1,4-butanedisulfonate is an orally active methyl group donor. S-Adenosyl-L-methionine 1,4-butanedisulfonate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine 1,4-butanedisulfonate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine 1,4-butanedisulfonate has the potential for, cancer, liver disease and osteoarthritis research[1][2][3].