GW 280264X

GW 280264X is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-alpha converting enzyme (ADAM17/TACE) and ADAM10 (IC50s = 8 and 11.5 nM, respectively). It inhibits TNF-alpha-induced cleavage of endomucin in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM. GW 280264X (1 and 10 µM) inhibits angiotensin-converting enzyme 2 (ACE2) ectodomain shedding induced by phorbol 12-myristate 13-acetate (PMA, Cay-10008014) in HEK-ACE2 cells. It reduces ACE2 shedding and prevents severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in HK-2 cells.Formal Name: N-[(5S)-5-[[(2R,3S)-3-(formylhydroxyamino)-2-(2-methylpropyl)-1-oxohexyl]amino]-6-oxo-6-(2-thiazolylamino)hexyl]-carbamic acid, penthylmethyl ester. CAS Number: 866924-39-2. Molecular Formula: C28H41N5O6S. Formula Weight: 575.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. SMILES: O=CN(O)[C@@H](CCC)[C@@H](CC(C)C)C(N[C@@H](CCCCNC(OCC1=CC=CC=C1)=O)C(NC2=NC=CS2)=O)=O. InChi Code: InChI=1S/C28H41N5O6S/c1-4-10-24(33(38)19-34)22(17-20(2)3)25(35)31-23(26(36)32-27-29-15-16-40-27)13-8-9-14-30-28(37)39-18-21-11-6-5-7-12-21/h5-7,11-12,15-16,19-20,22-24,38H,4,8-10,13-14,17-18H2,1-3H3,(H,30,37)(H,31,35)(H,29,32,36)/t22-,23+,24+/m1/s1. InChi Key: SKJLITFHSZNZMQ-SGNDLWITSA-N.