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Cat. No.: HY-112714

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GSK3532795

(Synonyms: BMS-955176)

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Based on 1 Customer Validation

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.

Purity: 98.0%
CAS No.: 1392312-45-6
Formula: C₄₂H₆₂N₂O₄S
Molecular Weight:691.02

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK3532795 Chemical Structure

CAS No.: 1392312-45-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

HIV-1

All HIV Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MT2	CC₅₀	13 μM Compound: 3; GSK3532795, BMS-955176	Cytotoxicity against human MT2 cells assessed as reduction in cell viability Cytotoxicity against human MT2 cells assessed as reduction in cell viability	[PMID: 36441509]
MT2	CC₅₀	13 μM Compound: 4; GSK3532795, BMS-955176	Cytotoxicity in human MT2 cells assessed as reduction in cell viability Cytotoxicity in human MT2 cells assessed as reduction in cell viability	[PMID: 36044257]
MT2	CC₅₀	9.2 nM Compound: 2; BMS-955176	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 27326328]
MT2	CC₅₀	9.2 μM Compound: 1; BMS-955176, GSK3532795	Cytotoxicity against human MT2 cells assessed as reduction in cell viability Cytotoxicity against human MT2 cells assessed as reduction in cell viability	[PMID: 30067361]
MT2	CC₅₀	9.2 μM Compound: 3; GSK3532795; BMS-955176	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 33508465]
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	3.9 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation	[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 K_ds 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1392312-45-6
Appearance Solid
Molecular Weight 691.02
Formula C₄₂H₆₂N₂O₄S
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
Synonyms

BMS-955176
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Regueiro-Ren A, et al. Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176). J Med Chem. 2018 Aug 23;61(16):7289-7313. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Purity & Documentation
References

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GSK3532795

All HIV Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

GSK3532795 Related Classifications

HY-112714 Related Classifications