PeptideDB

GAPDH-IN-1

CAS: 252212-58-1 F: C20H18N2O5 W: 366.37

GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC50 of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a coval
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Bioactivity 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].
Invitro 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. 0 --> GAPDH-IN-1 相关抗体: Western Blot Analysis[1] Cell Line:
CAS 252212-58-1
Formula C20H18N2O5
Molar Mass 366.37
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]. 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.