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  3. HIV
  4. GSK3532795

GSK3532795  (Synonyms: BMS-955176)

Cat. No.: HY-112714 Purity: ≥98.0%
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GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.

For research use only. We do not sell to patients.

GSK3532795 Chemical Structure

GSK3532795 Chemical Structure

CAS No. : 1392312-45-6

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Based on 1 publication(s) in Google Scholar

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Description

GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively[1].

IC50 & Target

EC50: 1.9 nM (HIV-1 WT), 10.2 nM (HIV-1 WT(human serum)), 2.7 nM (HIV-1 V370A), 13 nM (HIV-1 ΔV370)[1]
Cellular Effect
Cell Line Type Value Description References
MT2 EC50
1.9 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
1.9 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
10.2 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-lucife
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-lucife
[PMID: 27326328]
MT2 EC50
13 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
2 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
2.7 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
2.8 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
3.6 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
4.5 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
7.3 nM
Compound: 2; BMS-955176
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
In Vitro

GSK3532795 exhibits Kds of 3.2 ± 0.6, 4.3 ± 2.0, 6.5 ± 2.2 and 33.6 ± 5.9 nM for HIV WT, HIV V362I, HIV V370A, HIV ΔV370, respectively[1].

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

GSK3532795 Related Antibodies
Clinical Trial
Molecular Weight

691.02

Formula

C42H62N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1(C)C(C2=CC=C(C(O)=O)C=C2)=CC[C@@]3(C)[C@@]1([H])CC[C@]4(C)[C@]3([H])CC[C@@]5([H])[C@@]4(C)CC[C@]6(NCCN7CCS(CC7)(=O)=O)[C@]5([H])[C@H](C(C)=C)CC6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.59%

SDS (251 KB)

COA (250 KB) HNMR (279 KB) LCMS (260 KB)

Handling Instructions (2659 KB)
References
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GSK3532795 Related Classifications

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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:

GSK35327951392312-45-6BMS-955176GSK 3532795GSK-3532795BMS955176BMS 955176HIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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