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5.00653

Nef Hck Activation Inhibitor, B9

Synonym(s):

Nef Hck Activation Inhibitor, B9, Nef Dimerization Blocker, ( E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide, Nef Dimerization Blocker, (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide

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Size/SKUAvailabilityPrice
10 mg
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$197.00

About This Item

Empirical Formula (Hill Notation):
C16H11ClN6O3S
CAS Number:
1596216-24-8
Molecular Weight:
402.81
UNSPSC Code:
51111800
NACRES:
NA.77
PubChem Substance ID:
4553981
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light

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assay

≥98% (HPLC)

Quality Segment

100

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

orange

solubility

DMSO: 2.5 mg/mL

storage temp.

2-8°C

SMILES string

C1=CC(=CC(=C1)Cl)N=NC2=C(NN(C2=O)C(=S)N)C3=CC=C(C=C3)[N+](=O)[O-]

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)

InChI key

LEQSBTDRMOZWRP-UHFFFAOYSA-N

General description

A cell-permeable diphenylpyrazolo compound that is shown to disrupt HIV accessary protein Nef dimerization (IC50 = 3 µM in HEK293T cells) and prevent Nef-mediated Src family kinase (SFK) Hck activation (IC50 = 2.8 µM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn (IC50 >20 µM). Shown to effectively suppress HIV and SIV viral replication (IC50<0.3 µM in 9 d HIV-1 NL4-3-infected CEM-T4 cultures; IC50 = 1 µM in 5 d SIV ΔB670-infected CEM-174 cultures) and infectivity (45% and 50% inhibition against HIV-1 NL4-3 and SIV ΔB670, respectively, following 48 h 3 µM B9 treatment in TZM-bl reporter cells) in a Nef-dependent manner, being ineffective against the replication of Nef-defective HIV-1 mutant. Molecular docking studies predict a high-affinity B9-targeting site formed at the Nef dimerization interface and a low-affinity B9-binding site on each Nef monomer at the dimer interface periphery, with Asn126 contributing to both modes of binding. Consistently, in vitro binding studies reveal two B9 KD values of 1.72 nM and 860 nM toward full-length HIV-1 Nef and a complete loss of B9 binding toward Nef N126A/L/Q mutants.

Biochem/physiol Actions

Reversible: yes
Cell permeable: yes
Primary Target
Nef

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Emert-Sedlak, L.A., et al. 2013. Chem. Biol.20, 82.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Sigma-Aldrich

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E-64 Protease Inhibitor The E-64 Protease Inhibitor, also referenced under CAS 66701-25-5, controls the biological activity of E-64 Protease. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

Sigma-Aldrich

324890

E-64 Protease Inhibitor

description

-

description

-

description

-

description

The E-64 Protease Inhibitor, also referenced under CAS 66701-25-5, controls the biological activity of E-64 Protease. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

form

powder

form

solid

form

powder

form

solid

assay

≥98% (HPLC)

assay

≥97% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

200

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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