GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).

Product information

CAS Number: 732973-87-4

Molecular Weight: 354.83

Formula: C19H19ClN4O

Chemical Name: N-(4-chlorophenyl)-4-(1H-indol-4-yl)piperazine-1-carboxamide

Smiles: O=C(NC1C=CC(Cl)=CC=1)N1CCN(CC1)C1=CC=CC2NC=CC=21

InChiKey: VVVZKBOSNCHQEJ-UHFFFAOYSA-N

InChi: InChI=1S/C19H19ClN4O/c20-14-4-6-15(7-5-14)22-19(25)24-12-10-23(11-13-24)18-3-1-2-17-16(18)8-9-21-17/h1-9,21H,10-13H2,(H,22,25)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (352.28 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1 (glutamate-oxaloacetate transaminase 1 (GOT1)), for the maintenance of redox homeostasis and sustained proliferation. Small molecule inhibitors targeting this metabolic pathway may provide a novel way for cancer research. In the MDH coupled GOT1 enzymatic assay, GOT1 inhibitor-1 shows an inhibitory effect on GOT1 activity with an IC50 value of 8.2 uM.

References:

1. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678

Products are for research use only. Not for human use.