2. Anti-infection
  3. HIV
  4. GSK3532795

GSK3532795 是一种有效、可口服、第二代 HIV-1 成熟抑制剂，对 HIV-1 WT，HIV-1 WT(人血清)，HIV-1 V370A 和 HIV-1 ΔV370 的 EC50 值分别为 1.9，10.2，2.7 和 13 nM。

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GSK3532795

GSK3532795 Chemical Structure

CAS No. : 1392312-45-6

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1 mg ￥3350
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GSK3532795 相关抗体

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HIV HIV-1 HIV-2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

HIV-1

 

细胞效力
(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 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
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
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-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/40% human serum/27 mg/ml human serum albumin by dual-luciferase reporter assay
[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]
体外研究
(In Vitro)

GSK3532795 对 HIV WT、HIV V362I、HIV V370A、HIV ΔV370 的 Kd 分别为 3.2 ± 0.6、4.3 ± 2.0、6.5 ± 2.2 和 33.6 ± 5.9 nM[1]。

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

GSK3532795 相关抗体:
Clinical Trial
分子量

691.02

Formula

C42H62N2O4S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 99.59%

COA (287 KB) HNMR (279 KB) LCMS (260 KB)

产品使用指南 (1538 KB)
参考文献

GSK3532795 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称：
GSK3532795
目录号：
HY-112714
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