Hck-IN-1


Catalog No. Size PriceQuantity
M32021-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.

Product information

CAS Number: 1473404-51-1

Molecular Weight: 402.81

Formula: C16H11ClN6O3S

Chemical Name: 4-[2-(3-chlorophenyl)diazen-1-yl]-3-(4-nitrophenyl)-5-oxo-2,5-dihydro-1H-pyrazole-1-carbothioamide

Smiles: NC(=S)N1NC(=C(N=NC2=CC(Cl)=CC=C2)C1=O)C1C=CC(=CC=1)[N+]([O-])=O

InChiKey: LEQSBTDRMOZWRP-FMQUCBEESA-N

InChi: InChI=1S/C16H11ClN6O3S/c17-10-2-1-3-11(8-10)19-20-14-13(21-22(15(14)24)16(18)27)9-4-6-12(7-5-9)23(25)26/h1-8,21H,(H2,18,27)/b20-19+

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 12.5 mg/mL (31.03 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:

Hck-IN-1 (compound B9) shows weak activity against other Src-family members in vitro, with IC50 values >20 μM for c-Src, Lck and Lyn. B9 (1 μM; 8 days) completely inhibits Nef-dependent SFK activation at a concentration of 1.0 μM. Hck-IN-1 (0.1, 0.3, 1, 3 μM) also inhibits Nef-mediated enhancement of HIV-1 infectivity in a concentration-dependent manner in the reporter cell line, TZM-bl. Hck-IN-1 inhibits the replication of all eleven HIV-1 Nef chimeras with IC50 values of ~ 300 nM in CEM-T4 cells, demonstrating that the compound is broadly active against HIV replication supported by a wide range of HIV-1 Nef proteins.

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

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