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) exhibits a dose-dependent increase in the probe labeling of the 40 kDa protein^[1].
GAPDH-IN-1 (50 μM, 4 h) covalently reacts with Asp35 but not cysteine residues in GAPDH, stimulating the subsequent reaction of Cys152 with the iodoacetamide-based (IA) probe^[1].
GAPDH-IN-1 (25-50 μM, 24 h) enhances probe and GAPDH responses less in HEK293 cells than in cell lysates^[1].
GAPDH-IN-1 (0-100 μM, 24 h) displays a concentration-dependent inactivation of GAPDH in HEK293 cell lysates, with an IC₅₀ of 39.31 μM^[1].
GAPDH-IN-1 (0-100 μM) inhibits the viability of HEK293 cells, with an IC₅₀ of 50.64 μM^[1].
GAPDH-IN-1-GAPDH adduct can be reduced by the addition of excess NAD⁺, as evidenced by the band shifts of endogenous GAPDH in a silver-stained gel^[1].

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

366.37

C₂₀H₁₈N₂O₅

252212-58-1

C1(C2=CC(OCC3OC3)=CC=C2)=NN=C(C4=CC(OCC5OC5)=CC=C4)O1

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]