Bioactivity | SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance[1]. |
Target | IC50: 9.6 nM (NDM-1) |
Invitro | SA09-Cu (5-160 μg/mL; 24 h) 在40 μg/mL 时,使 Vero E6 和 L929 小鼠细胞的存活率高于 60%[1]。 SA09-Cu (2, 4, 8, 16 μg/mL; 24 h) 对活细胞 (E. coli-BL21-NDM-1 和 EC23) 中的 NDM-1 活性有明显的剂量依赖性的抑制作用 [1]. SA09-Cu 本身没有或只有轻微的抗菌活性 (MICs≥64 μg/mL)[1]。 |
Name | SA09-Cu |
CAS | 155641-16-0 |
Formula | C8H16CuN2O2S4 |
Molar Mass | 364.03 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Cheng Chen, et al. Dithiocarbamates combined with copper for revitalizing meropenem efficacy against NDM-1-producing Carbapenem-resistant Enterobacteriaceae. Bioorg Chem. 2022 Jan;118:105474. |