HIF-C2 --- HIF-2 Inhibitor

HIF-C2 is a potent and selective allosteric inhibitor of hypoxia inducible factor-2 (HIF-2). It binds within the internal cavity of HIF-2α PAS-B (Kd of 81 nM) and disrupts heterodimerization of the full-length HIF-2 transcription factor. HIF-C2 functions effectively as a HIF-2 inhibitor in living cells, disrupting HIF-2 DNA binding and inhibiting the transcription of its target genes. Moreover, HIF-C2 is selective for the HIF-2 isoform and has no activity to antagonize HIF-1. HIF-C2 provides an opportunity to delineate differences in HIF-1 and HIF-2 biology and serves as an entry point for development of HIF-2 inhibitor drugs for treating diseases, including renal cell carcinomas.

Product information

CAS Number: 1422955-31-4

Molecular Weight: 308.65

Formula: C12H6ClFN4O3

Synonym:

TC-S 7009

Chemical Name: N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine

Smiles: [O-][N+](=O)C1C2=NON=C2C=CC=1NC1C=C(Cl)C=C(F)C=1

InChiKey: CDQUJZKBRAFWNG-UHFFFAOYSA-N

InChi: InChI=1S/C12H6ClFN4O3/c13-6-3-7(14)5-8(4-6)15-10-2-1-9-11(17-21-16-9)12(10)18(19)20/h1-5,15H

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 50 mM

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:

HIF-C2 was used at 10 µM final concentration in vitro and in cellular assays.

References:

1. Scheuermann TH, et al. Allosteric inhibition of hypoxia inducible factor-2 with small molecules. (2013) Nat Chem Biol 9(4):271-6.
2. Rogers JL, et al. Development of Inhibitors of the PAS-B Domain of the HIF-2α Transcription Factor. (2013) J Med Chem. 56(4):1739-47.

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

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