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].
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer[1].
Ac-VRPR-AMC is a fluorogenic metacaspase substrate. Ac-VRPR-AMC can be used to tests metacaspase activity[1].
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].
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity[1][2].
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].
1,6,7-Trihydroxyxanthone is a potent anticancer agent. 1,6,7-Trihydroxyxanthone inhibits cell proliferation and induces cell Apoptosis. 1,6,7-Trihydroxyxanthone decreases Bmi-1 expressio and increases the protein levels expression of P14, P16[1].
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity[1].
NBI-961 is a potent NEK2 inhibitor that inhibits proteasomal degradation. NBI-961 induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells[1].
Apocynin-d3 is the deuterium labeled Apocynin[1]. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM[2][3][4].
KEA1-97 (KEA 1-97) is a small molecule that disrupts the interaction of thioredoxin with caspase 3; activates caspases, and induces apoptosis without affecting thioredoxin activity, impairs triple-negative breast cancer cell survival; impairs in vivo breast tumor xenograft growth.
Apoptosis inducer 6 (compound 4e) is an anticancer agent with a broad-spectrum anticancer activity. Apoptosis inducer 6 triggers cell death through the induction of apoptosis[1].
Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct[1][2].
S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].
Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively[1].
Rhapontin (Rhaponiticin), a component of rhubarb (Rheum officinale Baillon), induces apoptosis resulting in suppression of proliferation of human stomach cancer KATO III cells[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].
Zalypsis (PM00104) has anti-tumor activity. Zalypsis binds to DNA and shows cytotoxicity. Zalypsis inhibits cell cycle and transcription, and leads to double stranded DNA breaks[1][2].
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].
Anti-osteoporosis agent-1 (comp 4aa) is a potent replication protein A (RPA) inhibitor (IC50=18 µM) [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.
Bcl-2-IN-13 is a Bcl-2 inhibitor with an IC50 value of 17 nM. Bcl-2-IN-13 can be used in cancer research[1].
A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[1][2][3][4].
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.
D-Mannitol-13C is the 13C labeled D-Mannitol[1][2][3][4].