Nef-IN-B9

Research use only, not for human use.

Nef-IN-B9 (Nef inhibitor B9) is a small molecule that blocks Nef-dependent Hck activity with IC50 of 2.8 uM.

Nef-IN-B9 (Nef inhibitor B9) is a small molecule that blocks Nef-dependent Hck activity with IC50 of 2.8 uM, while the activity against Hck alone is >20 uM; also showes weak activity against other Src-family members with IC50 of >20 uM for c-Src, Lck and Lyn; blocks wild-type HIV-1 replication with IC50 of 100-300 nM, and blocks Nef-mediated SFK activation in HIV-infected cells; binds directly to Nef with Kd of 1.79 nM.

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. Western Blot Analysis Cell Line:CEM-T4 cells.Concentration:1 μM.Incubation Time:8 daysResult:Completely inhibited Nef-dependent SFK activation at a concentration of 1.0 μM.

——

Nef inhibitor B9

Microbiology/Virology

HIV

HIV

——

——

1473404-51-1

402.813

C16H11ClN6O3S

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (31.03 mM)

——

(E)-4-((3-chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide

(-20℃)

With Ice Pack

≥ 2 years