Thiazolobenzimidazole (Synonyms: NSC-625487)

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Thiazolobenzimidazole (NSC-625487) 是一种高效的非核苷类 HIV-1 逆转录酶 (HIV-1 reverse transcriptase) 抑制剂。Thiazolobenzimidazole 可抑制多种人类细胞系中 HIV 诱导的细胞死亡和病毒复制。

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Thiazolobenzimidazole Chemical Structure

CAS No. : 138226-12-7

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生物活性
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参考文献

生物活性

Thiazolobenzimidazole (NSC-625487) is a highly potent nonnucleoside HIV-1 reverse transcriptase inhibitor. Thiazolobenzimidazole inhibits HIV-induced cell killing and viral replication in a variety of human cell lines^[1].

IC₅₀ & Target^[1]

HIV-1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	50 μM Compound: TBZ	Cytotoxicity against CEM cells Cytotoxicity against CEM cells	[PMID: 17178227]
CCRF-CEM	CC₅₀	50 μM Compound: TBZ-1	Cytotoxicity against mock-infected CEM cells assessed as reduction of cell viability Cytotoxicity against mock-infected CEM cells assessed as reduction of cell viability	[PMID: 17349793]
CCRF-CEM	CC₅₀	50 μM Compound: TBZ-1	Cytotoxicity against human CEM cells by MTT assay Cytotoxicity against human CEM cells by MTT assay	[PMID: 18242784]
CCRF-CEM	EC₅₀	1.1 μM Compound: TBZ	Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced syncytium formation after 4 days Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced syncytium formation after 4 days	[PMID: 17178227]
CCRF-CEM	EC₅₀	1.1 μM Compound: TBZ-1	Antiviral activity against HIV1 3B-induced cytopathic effect in CEM cells assessed as inhibition of virus-induced syncytium formation Antiviral activity against HIV1 3B-induced cytopathic effect in CEM cells assessed as inhibition of virus-induced syncytium formation	[PMID: 17349793]
CCRF-CEM	EC₅₀	1.1 μM Compound: TBZ-1	Antiviral activity against HIV1 3B replication in human CEM cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay Antiviral activity against HIV1 3B replication in human CEM cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay	[PMID: 18242784]
CCRF-CEM	EC₅₀	1.73 μM Compound: TBZ	Concentration required to protect CEM cells against Mutant E138K Strain Concentration required to protect CEM cells against Mutant E138K Strain	[PMID: 15857150]
CCRF-CEM	EC₅₀	13.8 μM Compound: TBZ	Concentration required to protect CEM cells against Mutant Y181C Strain Concentration required to protect CEM cells against Mutant Y181C Strain	[PMID: 15857150]
CCRF-CEM	EC₅₀	15.6 μM Compound: TBZ	Concentration required to protect CEM cells against Mutant K103N Strain Concentration required to protect CEM cells against Mutant K103N Strain	[PMID: 15857150]
CCRF-CEM	EC₅₀	3.12 μM Compound: TBZ	Concentration required to protect CEM cells against Mutant L100I Strain Concentration required to protect CEM cells against Mutant L100I Strain	[PMID: 15857150]
CCRF-CEM	EC₅₀	4.16 μM Compound: TBZ	Concentration required to protect CEM cells against Mutant Y188H Strain Concentration required to protect CEM cells against Mutant Y188H Strain	[PMID: 15857150]
CEM-SS	EC₅₀	0.52 mM Compound: TZB	In vitro 50% cellular protection of CEM-SS cells from HIV-1 induced cytopathicity. In vitro 50% cellular protection of CEM-SS cells from HIV-1 induced cytopathicity.	[PMID: 9435891]
MT4	CC₅₀	19.2 μM Compound: TBZ	Cytotoxicity against MT4 cells Cytotoxicity against MT4 cells	[PMID: 17178227]
MT4	CC₅₀	19.2 μM Compound: TBZ-1	Cytotoxicity against mock-infected MT4 cells assessed as reduction of cell viability Cytotoxicity against mock-infected MT4 cells assessed as reduction of cell viability	[PMID: 17349793]
MT4	CC₅₀	19.2 μM Compound: TBZ-1	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 18242784]
MT4	CC₅₀	19.2 μM Compound: TBZ1	Cytotoxicity to reduce MT-4 cell viability by 50% Cytotoxicity to reduce MT-4 cell viability by 50%	[PMID: 11425562]
MT4	CC₅₀	50 μM Compound: TBZ	Cytotoxic concentration required to reduce MT-4 cell viability Cytotoxic concentration required to reduce MT-4 cell viability	[PMID: 15857150]
MT4	EC₅₀	0.35 μM Compound: TBZ	Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days	[PMID: 17178227]
MT4	EC₅₀	0.35 μM Compound: TBZ-1	Antiviral activity against HIV1 3B-induced cytopathic effect in MT4 cells assessed as inhibition of virus-induced syncytium formation Antiviral activity against HIV1 3B-induced cytopathic effect in MT4 cells assessed as inhibition of virus-induced syncytium formation	[PMID: 17349793]
MT4	EC₅₀	0.35 μM Compound: TBZ-1	Antiviral activity against HIV1 3B replication in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay Antiviral activity against HIV1 3B replication in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay	[PMID: 18242784]
MT4	EC₅₀	0.352 μM Compound: TBZ1	Anti-HIV activity to reduce HIV-1-induced cytopathic effect by 50% in MT-4 cells against HIV-1 IIIB Anti-HIV activity to reduce HIV-1-induced cytopathic effect by 50% in MT-4 cells against HIV-1 IIIB	[PMID: 11425562]
MT4	EC₅₀	1.1 μM Compound: TBZ	Concentration required to reduce HIV-1-induced cytopathic effect in MT-4 cells Concentration required to reduce HIV-1-induced cytopathic effect in MT-4 cells	[PMID: 15857150]
MT4	EC₅₀	1.39 μM Compound: TBZ	Compound was tested for inhibition of the cytopathic effects of HIV-1 (IIIB) in MT-4 cells Compound was tested for inhibition of the cytopathic effects of HIV-1 (IIIB) in MT-4 cells	[PMID: 15857150]
MT4	EC₅₀	1100 nM Compound: 81; NSC625487	Antiviral activity against HIV1 infected in human MT4 cells assessed as protection against HIV-1 induced cytopathicity by MTT assay Antiviral activity against HIV1 infected in human MT4 cells assessed as protection against HIV-1 induced cytopathicity by MTT assay	[PMID: 26509831]
MT4	IC₅₀	14.6 μM Compound: TBZ1	Evaluated for the inhibition of replication of HIV-1 IIIB or HIV-2 (ROD) in MT-4 cells by using [3H]-dGTP as the radiolabeled substrate Evaluated for the inhibition of replication of HIV-1 IIIB or HIV-2 (ROD) in MT-4 cells by using [3H]-dGTP as the radiolabeled substrate	[PMID: 11425562]

分子量

288.32

Formula

C₁₅H₁₀F₂N₂S

CAS 号

138226-12-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Buckheit RW Jr, et al. Thiazolobenzimidazole: biological and biochemical anti-retroviral activity of a new nonnucleoside reverse transcriptase inhibitor. Antiviral Res. 1993 Jul;21(3):247-65.

Thiazolobenzimidazole 相关分类

Infection

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:

Thiazolobenzimidazole138226-12-7NSC-625487NSC625487NSC 625487Reverse TranscriptaseHIVHuman immunodeficiency virusHIV-1 reverse transcriptase inhibitorInhibitorinhibitorinhibit

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上海工商

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Thiazolobenzimidazole (Synonyms: NSC-625487)

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Thiazolobenzimidazole (Synonyms: NSC-625487)

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Thiazolobenzimidazole 相关分类

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