GAPDH-IN-1 

GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC₅₀ of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD⁺, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine^[1].

GAPDH-IN-1 (1.6-50 μM) 剂量依赖性地增加 40 kDa 蛋白探针标记^[1]。
GAPDH-IN-1 (50 μM, 4 h) 与 GAPDH 中Asp35 而不是半胱氨酸残基发生共价反应，刺激 Cys152 随后与 iodoacetamide-based (IA) 探针发生反应^[1]。
GAPDH-IN-1 (25-50 μM, 24 h) 在 HEK293 细胞中对探针和 GAPDH 反应的增强程度低于在细胞裂解物中的增强程度^[1]。
GAPDH-IN-1 (0-100 μM, 24 h) 在 HEK293 细胞裂解液中浓度依赖性地失活 GAPDH，IC₅₀ 为 39.31 μM^[1]。
GAPDH-IN-1 (0-100 μM) 可抑制 HEK293 细胞的活力，IC₅₀ 为 50.64 μM^[1]。
GAPDH-IN-1-GAPDH 加合物可通过添加过量 NAD⁺ 而减少，这可以从银染色凝胶中内源性 GAPDH 的条带移动得到证明^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

366.37

C₂₀H₁₈N₂O₅

252212-58-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jung Y, et al. Discovery of Non-Cysteine-Targeting Covalent Inhibitors by Activity-Based Proteomic Screening with a Cysteine-Reactive Probe. ACS Chem Biol. 2022 Feb 18;17(2):340-347.  [Content Brief]