L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells[1][2][3].
Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
Luteolin is a falconoid compound, which exhibits anticancer properties.IC50 value:Target: A natural for anticancer.In vitro: Luteolin exerted an anticancer effect against NCI-H460 cells through Sirt1-mediated apoptosis and the inhibition of cell migration [1]. The treatment of luteolin upregulated the expression levels of transforming growth factor β1 (TGF-β1), p21WAF1/CIP1, p27KIP1, Smad4, and Fas in HCC cells. Luteolin induced apoptotic cell death in Hep3B cells while caused G1 arrest in HepG2 cells. And it induces apoptosis from G1 arrest via three signaling pathways of TGF-β1, p53, and Fas/Fas-ligand in HCC cells [2].In vivo: The study of the effect of Luteolin on the improvement of cancerous cachexia in model mice showed that luteolin can improve the symptoms of cancer cachexia model mice.The mechanism may be related to inhibition of proteasome and calcium activated protease activity and lower the levels of cytokines [3].
Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells[1].
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
Oxcarbazepine-D4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis[1][2][3].
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2].
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition[1].
HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells[1][2][3].
Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural compound present in Cinchona bark. Cinchonine hydrochloride activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells[1].
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics[1].Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential drug candidate for treating triple-negative breast cancer (TNBC)[2].
Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin (Terinin) induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage[1][2][3][4].
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth[1].
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model[1].
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L[1][2].
Formoxanthone A is an apoptosis inducing compound that can significantly reduce the viability of HeLa cells at 25 μM[1].
Cytochrome C is a multi-functional enzyme involving in life and death decisions of the cell. Cytochrome C is essential in mitochondrial electron transport and intrinsic type II apoptosis[1].
Biatractylolide is a compound isolated from the ethyl acetate extract of Atractylodes macrocephala. Biatractylolide has antitumor and antioxidant activities. Biatractylolide improves cell viability, inhibits the apoptosis of cells induced by glutamate, and reduces the activity of LDH. Biatractylolide has neuroprotective effects[1].
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM[1].
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity[1][2][3][4][5].
Chrysosplenol D is a methoxy flavonoid that induces ERK1/2-mediated apoptosis in triple negative human breast cancer cells. Chrysosplenol D also exhibits anti-inflammatory and moderate antitrypanosomal activities[1][2][3][4].
Bleomycin A5 hydrochloride is an anti-neoplastic glycoprotein antibiotic. Bleomycin A5 suppresses Drp1‑mediated mitochondrial fission and induces apoptosis in human nasal polyp‑derived fibroblasts[1][2].
Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3[1].
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis[1].
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death[1].
Duocarmycin A, which is one of well-known antitumor antibiotics, efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels[1].
Ac-LEHD-AFC is a fluorescent substrate for caspase-9, can be used to assess the activity of caspase[1].