TAS4464 hydrochloride

• CAT Number: I018983
• CAS Number: 1848959-11-4
• Molecular Formula: C₂₁H₂₄ClFN₆O₆S
• Molecular Weight: 542.97
• Purity: ≥95%
• Target: NEDD8-activating Enzyme
• Storage: Store at -20°C
• IUPAC Name: 4-amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]oxolan-2-yl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]pyrrolo[2,3-d]pyrimidine;hydrochloride
• InChI: InChI=1S/C21H23FN6O6S.ClH/c1-2-33-14-5-3-4-13(22)12(14)7-6-11-9-28(20-16(11)19(23)25-10-26-20)21-18(30)17(29)15(34-21)8-27-35(24,31)32;/h3-5,9-10,15,17-18,21,27,29-30H,2,8H2,1H3,(H2,23,25,26)(H2,24,31,32);1H/t15-,17-,18-,21-;/m1./s1
• InChIKey: CDCFJYCKNAWPTL-WVAMHNCPSA-N
• SMILES: CCOC1=C(C(=CC=C1)F)C#CC2=CN(C3=NC=NC(=C23)N)C4C(C(C(O4)CNS(=O)(=O)N)O)O.Cl

TAS4464 hydrochloride（Cat No.:I018983） is a remarkable inhibitor of NEDD8 activating enzyme (NAE), known for its high potency and selectivity. With an impressive IC50 value of 0.955 nM, it demonstrates robust inhibition of NAE activity. NAE plays a crucial role in the process of NEDD8 conjugation, which regulates protein degradation and cellular signaling pathways. By specifically targeting NAE, TAS4464 hydrochloride shows promise as a therapeutic agent for diseases associated with dysregulated protein degradation, such as cancer.

Reference

[1]. Yoshimura C, et al. TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, suppresses neddylation and shows antitumor activity in diverse cancer models. Mol Cancer Ther. 2019 May 15.