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. This blocks the interaction between the hRRM1 and hRRM2 subunits and interferes with the assembly of the active hRRM1/hRRM2 complex of RNR. 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.
Chemical | |
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CAS Num | 1190932-38-7 |
Chemical Formula | C22H16N2O5S |
Molecular Weight | 420.439 |
IUPAC Chemical Name | N-(4-(3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide |
Exact Mass | 420.078 |
Elemental Analysis | C, 62.85; H, 3.84; N, 6.66; O, 19.03; S, 7.63 |
Synonym | COH29; COH-29; COH 29. |
Solubility | Soluble in DMSO, not in water |
SMILES Code | OC1=C(O)C=C(C(NC2=NC(C3=CC(O)=C(O)C=C3)=C(C4=CC=CC=C4)S2)=O)C=C1 |
Biological | |
Targets and Effects | ribonucleotide reductase inhibitor |
Pathways | Apoptosis |
Physical | |
Appearance | Solid powder |
Purity | >98% (or refer to the Certificate of Analysis) |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life | >2 years if stored properly |
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