(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1].
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis[1].
Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation[1].
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].
Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
Dasatinib D8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.
CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity[1][2].
Hydroxy-PP-Me is a potent and specific CBR1 inhibitor with an IC50 of 759 nM. Hydroxy-PP-Me inhibits serum-withdrawal-induced apoptosis. Hydroxy-PP-Me increases As2O3-induced apoptotic cell death compared with As2O3 alone[1][2].
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BWa,respectively [1]. T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates[1]. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides[1]. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues[2].
Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation[1][2].
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].
Antitumor agent-100 hydrochloride (compound A6), an apoptosis inducer and molecular glue, shows superior anti-tumor activity[1].
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis[1].
D-Mannitol-d1 is the deuterium labeled D-Mannitol.
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis[1][2].
Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Furazolidone-d4 is deuterium labeled Furazolidone.
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis[1][2].
Tanshinone IIB is a major active constituent of the roots of Salvia miltiorrhiza (Danshen) widely used for the research of stroke and coronary heart disease in Asian countries. Tanshinone IIB has a neuroprotective effect via inhibition of apoptosis[1].
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM)[1][2].
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis[1][2].
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability[1].
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis[1].
Rosamultic acid is an A-ring contracted triterpene, that can be isolated from the roots of Rosa rnultiflora. Rosamultic acid inhibits gastric cancer cells proliferation by inducing Apoptosis mediated through cell cycle arrest, downregulation of cell cycle related protein expressions, inhibition of cell migration, DNA damage, and activation of caspases[1][2].
Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research[1].
Genistein, a soy isoflavone, is a multiple tyrosine kinases inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes[1].
Garivulimab (BGB-A333) is a humanized IgG1-variant monoclonal antibody that specifically targets and binds to PD-L1. Garivulimab selectively blocks the interaction of PD-L1 and PD-1. Garivulimab has antitumor activity[1].