gst-p

Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

Ezatiostat TFA (TLK199) is a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity.

Methyl propyl disulfide is a natural compound containing volatile sulfur produced in garlic and onions. Methyl propyl disulfide displays an anticaner effect.

GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50 values of 1.4 μM for GSTP1-1, 16.3 μM for GSTM1, and 3.6 μM for GSTA2.

NBDHEX is a potent inhibitor of glutathione S-transferase P1-1 (GSTP1-1) .

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

Ezatiostat hydrochloride (TLK199 HCl) is an effective inhibitor of glutathione S-transferase. Ezatiostat hydrochloride is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GSTP1-1.

LAS17 is a selective and highly effective inhibitor of glutathione S-transferase Pi (GSTP1), which inhibits GSTP1 activity in vitro in a concentration-dependent manner. LAS17 has anti-tumor activity and inhibits breast cancer cell growth.

Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

NSC15520 is a replication protein A (RPA) inhibitor that inhibits the binding of Rad9-GST and p53-GST fusion proteins to the N-terminal DNA-binding domain (DBD) of RPA, inhibits helical destabilization of double-stranded DNA (dsDNA) oligonucleotides, and can be used to study DNA damage repair.

GSTP1-1 Inhibitor 1 (compound 6b) is an irreversible, long-acting inhibitor of glutathione S-transferase with a specific focus on GSTP 1-1, exhibiting an IC 50 of 21 μM. As GSTP 1-1 plays a crucial role in tumor suppression, this compound shows promising potential for anticancer activity [1].

740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

p53-MDM2-IN-6, an LSM-83177 hydrazone analog, acts as an efficacious p53-MDM2 inhibitor with an IC50 of 11.08 µg/mL. This compound inhibits the p53-MDM2 interaction leading to an increase in p-53 levels while concurrently decreasing GST enzyme expression. It halts the cell cycle at the S phase and induces early and late apoptosis (Apoptosis), exhibiting antiproliferative activity against the HT29 cell line with an IC50 of 10.44 µg/mL. p53-MDM2-IN-6 holds promise for research in colorectal cancer.

Coniferyl ferulate is a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis. It shows strong inhibition of human placental GST (IC50: 0.3 μM). It also reverses multidrug resistance and downregulates P-glycoprotein.

AP23464 represents a highly specialized ATP-based small molecule tyrosine kinase inhibitor specifically engineered to target the catalytic domain of Abl and Src kinases along with the Kit receptor with exceptional inhibitory potency and selectivity, effectively facilitating the measurable blockade of phosphorylation-mediated signaling across various preclinical experimental models to evaluate the suppression of oncogenic driver activities during strictly monitored laboratory observation periods and biochemical investigations to ensure high experimental sensitivity.

Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can significantly increased the activities of epoxide hydrase and glutathione-S-transferase but cause reduc

740 Y-P (740YPDGFR) is a PI3K activator with cell permeability. 740 Y-P binds GST fusion proteins containing the N-and C-terminal SH2 domains of p85.