T7940

Milnacipran (1S-cis) hydrochloride (Levomilnacipran Hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI), treatment of fibromyalgia.

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with an IC50 of 37 nM, and it also inhibits MCF-7 and HCT 116 cancer cell lines with IC50 values of 10.56 μM and 7.07 μM, respectively [1].

Tyrosinase-IN-13 (compound 3c), derived from Flurbiprofen, serves as a potent non-competitive inhibitor of tyrosinase with IC50 and Ki values of 68 μM and 36.3 μM, respectively. It exhibits cytotoxicity against several cancer cell lines, including hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) [1].

α-Amylase/α-Glucosidase-IN-4 (compound 5), a dual inhibitor targeting α-amylase (Amylases) and α-glucosidase (Glucosidase), exhibits potent inhibition with IC50 values of 1.10 μM and 0.15 μM respectively, and is noted for its potential antidiabetic activity [1].

VEGFR-2-IN-36 (compound 15) is a potent VEGFR-2 inhibitor with an IC50 value of 0.067 μM and acts as an apoptosis inducer with demonstrated anticancer efficacy, modulating apoptotic pathways by upregulating BAX and downregulating Bcl-2, leading to cytotoxic effects on cancer cell lines, including MCF-7 (IC50 = 0.42 μM) and HepG2 (IC50 = 0.22 μM) [1].

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis. It exhibits anti-cancer activity in triple-negative breast cancer (TNBC) cells and patient-derived organoids, making it useful for TNBC research, including cases with or without BRCA1 mutations [1].

HL23 is a histone deacetylase (HDAC) inhibitor that effectively targets hepatocellular carcinoma (HCC). It promotes acetylation at the TXNIP promoter and increases TXNIP expression, modulating potassium channel activity and inducing TXNIP-dependent potassium deficiency. Additionally, HL23 impedes HCC progression and spread, demonstrating greater potency when combined with Sorafenib than the Sorafenib and Vorinostat duo [1].

KGP591, a tubulin polymerization inhibitor with an IC50 of 0.57 µM, effectively induces G2/M arrest, inhibits cell migration, and disrupts microtubule structure and cell morphology in MDA-MB-231 cells. Additionally, it demonstrates antitumor activity in an orthotopic kidney cancer model (RENCA) [1].

Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when administered orally. It has been shown to be effective in vivo using a mouse model of staphylococcal sepsis [1].