rnr inhibitor coh 29

Menin-MLL Inhibitor 29 (Compound C1) is a Menin-MLL protein-protein interaction (PPI) inhibitor that demonstrates high affinity to Menin with a dissociation constant (K D) of 138 nM and impedes Menin's interaction with Menin-binding motif 1 (MBM1), as evidenced by an inhibition constant (IC 50) of 46 nM. Additionally, it exhibits anti-proliferative activity against HepG2 and Hep3B hepatoma cell lines with IC 50 values of 0.31 μM and 0.71 μM, respectively, and has been shown to inhibit tumor growth [1].

HIV-1 inhibitor-29 is a potent inhibitor of HIV-1 and acts against HIV-1 IIIB (EC50: 2.18 μM). HIV-1 inhibitor-29 shows high resistance to the F227L/V106A strain with an EC50 value of 0.974 μM. HIV-1 inhibitor-29 showed low cytotoxicity against MT-4 cells with a CC50 value of 211 μM. HIV-1 inhibitor-29 can be used in AIDS research.

KRAS G12C inhibitor 29 is an inhibitor of KRAS G12C and can be used to study cancer.

Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor that inhibits tubulin assembly and bounds in the colchicine site (IC 50 = 1.2 μM). Tubulin inhibitor 29 exhibits antiproliferative effects with an IC 50 value of 7.5 μM for MCF-7 cells. [1].

COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis.