compound 8h

Compound 8H is an inducer of G2/M-phase cell cycle arrest and cell death in cancer cell lines.

TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.

α-Glucosidase-IN-47 (compound 8H) is a non-competitive inhibitor of α-glucosidase, with an IC50 of 38.2 μM and a Ki of 38.2 µM. It is applicable for diabetes research.

SARS-CoV-2-IN-71 (compound 8h) is an effective inhibitor of SARS-CoV-2, demonstrating antiviral activity by targeting multiple stages of coronavirus replication. It exhibits its effects by simultaneously acting on 3CLpro and TMPRSS2.

USP1-IN-9 (Compound 1m) is a reversible and non-competitive inhibitor of ubiquitin-specific protease (USP1) with an IC50 value of 8.8 nM. It is synthesized based on the structures of ML323 and KSQ-4279 as a pyrido[2,3-d]pyrimidin-7(8H)-one derivative. USP1-IN-9 exhibits excellent inhibition of USP1/UAF and demonstrates strong antiproliferative effects on breast cancer cells. When combined with the PARP inhibitor olaparib, USP1-IN-9 enhances the cytotoxic effect on MDA-MB-436/OP cells. USP1-IN-9 holds potential for research in the field of cancer.

PARP10/15-IN-2 (Compound 8h) is a dual inhibitor of PARP10 and PARP15, with IC50 values of 0.15 μM and 0.37 μM, respectively. It can penetrate cells and prevent apoptosis [1].

Antiparasitic agent-5 (compound 8h) exhibits potent selectivity against Leishmania infantum (L. infantum) with an IC50 value of 2.50 μM and displays cytotoxic effects on HepG2 cells with a CC50 value of 6.78 μM [1].

2,6-Dibromo-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one is a useful organic compound for research related to life sciences. The catalog number is T64430 and the CAS number is 1415560-29-0.

1,2,6,7-Tetrahydro-8H-indeno[5,4-b]furan-8-one is a useful organic compound for research related to life sciences. The catalog number is T65555 and the CAS number is 196597-78-1.

(R)-tert-Butyl (4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-yl)carbamate is a useful organic compound for research related to life sciences and the catalog number is T65597.

(2Z)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazine-7(8H)-yl]-1-(2,4,5-trifluorophenyl)but-2-en-2-amine is a useful organic compound for research related to life sciences. The catalog number is T66986 and the CAS number is 767340-03-4.

1-(3-(Trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butane-1,3-dione is a useful organic compound for research related to life sciences. The catalog number is T67692 and the CAS number is 764667-65-4.

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1/M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].

MET/PDGFRA-IN-2 (compound 8h) is an inhibitor of MET and PDGFRA proteins that promotes apoptosis and impedes proliferation of MET-positive cells with IC50 values of 9.7, 6.1, 12.0, 11.5, 8.6, and 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, and K562 cells, respectively [1].

Compound 8h, also known as SARS-CoV-2-IN-43, is a powerful inhibitor effective in obstructing the replication of SARS-CoV-2, exhibiting significant antiviral activity [1].

Anticancer agent 154 (Compound 8h) enhances reactive oxygen species production, causes mitochondrial damage, and promotes cell apoptosis and DNA damage. It triggers ferroptosis by depleting GSH, diminishing GPX4 expression, and escalating lipid peroxidation. Additionally, it effectively suppresses the proliferation of various cancer cells (HT29, H1975, A549, and MCF-7) with IC50 values ranging from 1.0 to 1.9 μM [1].

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293 cells. It is utilized in congestive heart failure (HF) research [1].

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.