2. Protein Tyrosine Kinase/RTK Anti-infection
  3. Src HIV
  4. Hck-IN-1

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.

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Hck-IN-1 Chemical Structure

Hck-IN-1 Chemical Structure

CAS No. : 1473404-51-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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Hck-IN-1 Related Antibodies

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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[1].

IC50 & Target[1]

HIV-1 Nef

100-300 nM (IC50)

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[1].
B9 (1 μM; 8 days) completely inhibits Nef-dependent SFK activation at a concentration of 1.0 μM[1].
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[1].
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[1].

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

Hck-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: CEM-T4 cells
Concentration: 1 μM
Incubation Time: 8 days
Result: Completely inhibited Nef-dependent SFK activation at a concentration of 1.0 μM.
Molecular Weight

402.81

Formula

C16H11ClN6O3S
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

S=C(N1N=C(C2=CC=C([N+]([O-])=O)C=C2)C(/N=N/C3=CC=CC(Cl)=C3)=C1O)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (31.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4826 mL 12.4128 mL 24.8256 mL
5 mM 0.4965 mL 2.4826 mL 4.9651 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.53%

COA (255 KB) HNMR (231 KB) LCMS (135 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4826 mL 12.4128 mL 24.8256 mL 62.0640 mL
5 mM 0.4965 mL 2.4826 mL 4.9651 mL 12.4128 mL
10 mM 0.2483 mL 1.2413 mL 2.4826 mL 6.2064 mL
15 mM 0.1655 mL 0.8275 mL 1.6550 mL 4.1376 mL
20 mM 0.1241 mL 0.6206 mL 1.2413 mL 3.1032 mL
25 mM 0.0993 mL 0.4965 mL 0.9930 mL 2.4826 mL
30 mM 0.0828 mL 0.4138 mL 0.8275 mL 2.0688 mL
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Hck-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hck-IN-11473404-51-1SrcHIVHuman immunodeficiency virusdiphenylpyrazoloNef-dependentHckNef:HckNefreplicationAsn126anti-retroviralInhibitorinhibitorinhibit

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