BML-277(Synonyms: Chk2 Inhibitor II)

发表于2024年4月10日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BML-277 (Synonyms: Chk2 Inhibitor II) 纯度: 98.49%

BML-277 是一种选择性的检测点激酶 2 (Chk2) 抑制剂，IC₅₀ 为 15 nM。

BML-277 Chemical Structure

CAS No. : 516480-79-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥818	In-stock
10 mg	￥744	In-stock
50 mg	￥2976	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

BML-277 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Cell Cycle/DNA Damage Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Targeted Diversity Library

生物活性

BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC₅₀ of 15 nM.

IC₅₀ & Target^[1]

Chk2

15 nM (IC₅₀)

体外研究
(In Vitro)

BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4⁺ and CD8⁺ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC₅₀ of 3−7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theK_m of ATP for Chk2 is determined to be 99 μM and the K_i for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

363.80

Formula

C₂₀H₁₄ClN₃O₂

CAS 号

516480-79-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 22.22 mg/mL (61.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7488 mL	13.7438 mL	27.4876 mL
5 mM	0.5498 mL	2.7488 mL	5.4975 mL
10 mM	0.2749 mL	1.3744 mL	2.7488 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (4.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.

Kinase Assay ^[1]	Activity of inhibitors of chk2 is determined by incubating inhibitory compounds with recombinant full-length chk2: 5 nM recombinant human Chk2, 50 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl₂, 25 μM synthetic peptide substrate (biotin-SGLYRSPSMPENLNRPR, 1 μM ATP, 50 μCi/mL [γ-³³P] ATP, and a protease inhibitor mixture. The reaction mixtures are incubated at 37°C for 3 h, and the peptide substrate is captured on streptavidin conjugated to agarose beads. The agarose beads are washed repeatedly with a 0.1% solution of Tween-20 in phosphate-buffered saline, pH 7.4. Enzyme activity at different BML-277 concentrations (6.25, 12.5, 25, 50, 100, and 200 nM) is determined by measuring the amount of radioactive phosphate bound to the substrate peptide by scintillation counting. In kinetic experiments ATP concentration is varied while the ratio between unlabeled and [γ-³³P] labeled ATP is kept constant. Reactions are stopped at different time points by addition of 50 mM cold ATP and samples are kept on ice during further processing^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	To determine the radioprotective effect of Chk2 inhibitors, purified T-cells are incubated at 100 000 cells per well in BML-277 (10^2.5 nM, 1 μM, 10^0.5 μM, 10 μM, and 10^1.5 μM) or vehicle (DMSO) at varying concentrations in 96-well stripwells for 1 h. Cells are then exposed to a dose of 0 or 10 Gy gamma irradiation from a ¹³⁷Cs source at a dose rate of 3.65 Gy/min and then returned to the incubator for a further 24 h. Cells are stained with Annexin V-FITC and propidium iodide, according to the manufacturers protocol. Apoptotic and surviving cells are quantitated with a FACSCalibur FACS machine. Data are reported as percent recovery-or the number of survivors from treatment groups minus the number of cells surviving in the irradiated control group divided by the number of surviving cells in the untreated control groups^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.

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Chk1-IN-5

发表于2024年1月25日由上海金畔生物科技有限公司

Chk1-IN-5

Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化，并在结肠癌异种移植模型中抑制肿瘤生长。

Chk1-IN-5 Chemical Structure

CAS No. : 2120398-39-0

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100 mg		Check price and availability
250 mg		Check price and availability

* Please select Quantity before adding items.

生物活性

Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model^[1].

IC₅₀ & Target^[1]

Chk1

体外研究
(In Vitro)

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells^[1].
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T_1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V_ss=6.4 L/kg; AUC=4531 ng/ml•h)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Baib/c nude mice with HT-29 colon cancer cells^[1]
Dosage:	40 mg/kg
Administration:	IV; twice a week for 21 days
Result:	Inhibited tumor growth.

Animal Model:	Male SD rats (280-350 g)^[1]
Dosage:	10 mg/kg
Administration:	Via tail vein intravenous injection
Result:	Displayed a longer half-life (T_1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V_ss=6.4 L/kg; AUC=4531 ng/ml•h).

分子量

383.38

Formula

C₁₈H₁₈FN₇O₂

CAS 号

2120398-39-0

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.

参考文献

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Chk1-IN-5

发表于2024年1月25日由上海金畔生物科技有限公司

Chk1-IN-5

Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化，并在结肠癌异种移植模型中抑制肿瘤生长。

Chk1-IN-5 Chemical Structure

CAS No. : 2120398-39-0

规格		是否有货
100 mg		Check price and availability
250 mg		Check price and availability

* Please select Quantity before adding items.

生物活性

Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model^[1].

IC₅₀ & Target^[1]

Chk1

体外研究
(In Vitro)

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Baib/c nude mice with HT-29 colon cancer cells^[1]
Dosage:	40 mg/kg
Administration:	IV; twice a week for 21 days
Result:	Inhibited tumor growth.

Animal Model:	Male SD rats (280-350 g)^[1]
Dosage:	10 mg/kg
Administration:	Via tail vein intravenous injection
Result:	Displayed a longer half-life (T_1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V_ss=6.4 L/kg; AUC=4531 ng/ml•h).

分子量

383.38

Formula

C₁₈H₁₈FN₇O₂

CAS 号

2120398-39-0

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.

参考文献

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Chk1-IN-5

发表于2024年1月25日由上海金畔生物科技有限公司

Chk1-IN-5

Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化，并在结肠癌异种移植模型中抑制肿瘤生长。

Chk1-IN-5 Chemical Structure

CAS No. : 2120398-39-0

规格		是否有货
100 mg		Check price and availability
250 mg		Check price and availability

* Please select Quantity before adding items.

生物活性

Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model^[1].

IC₅₀ & Target^[1]

Chk1

体外研究
(In Vitro)

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Baib/c nude mice with HT-29 colon cancer cells^[1]
Dosage:	40 mg/kg
Administration:	IV; twice a week for 21 days
Result:	Inhibited tumor growth.

Animal Model:	Male SD rats (280-350 g)^[1]
Dosage:	10 mg/kg
Administration:	Via tail vein intravenous injection
Result:	Displayed a longer half-life (T_1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V_ss=6.4 L/kg; AUC=4531 ng/ml•h).

分子量

383.38

Formula

C₁₈H₁₈FN₇O₂

CAS 号

2120398-39-0

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.

参考文献

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Chk1-IN-6

发表于2023年12月11日由上海金畔生物科技有限公司

Chk1-IN-6

Chk1-IN-6 是一种强效、选择性和口服生物利用度 CHK1 候选抑制剂。

Chk1-IN-6 Chemical Structure

CAS No. : 2428423-77-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

IC₅₀ & Target

Chk1

分子量

365.36

Formula

C₁₆H₁₈F₃N₇

CAS 号

2428423-77-0

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.

参考文献

[1]. Jin T, et al. Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile. J Med Chem. 2021 Oct 28;64(20):15069-15090.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Chk1-IN-6

发表于2023年12月11日由上海金畔生物科技有限公司

Chk1-IN-6

Chk1-IN-6 是一种强效、选择性和口服生物利用度 CHK1 候选抑制剂。

Chk1-IN-6 Chemical Structure

CAS No. : 2428423-77-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

IC₅₀ & Target

Chk1

分子量

365.36

Formula

C₁₆H₁₈F₃N₇

CAS 号

2428423-77-0

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.

参考文献

[1]. Jin T, et al. Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile. J Med Chem. 2021 Oct 28;64(20):15069-15090.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Chk1-IN-6

发表于2023年12月10日由上海金畔生物科技有限公司

Chk1-IN-6

Chk1-IN-6 是一种强效、选择性和口服生物利用度 CHK1 候选抑制剂。

Chk1-IN-6 Chemical Structure

CAS No. : 2428423-77-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

IC₅₀ & Target

Chk1

分子量

365.36

Formula

C₁₆H₁₈F₃N₇

CAS 号

2428423-77-0

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.

参考文献

[1]. Jin T, et al. Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile. J Med Chem. 2021 Oct 28;64(20):15069-15090.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHK1 inhibitor(Synonyms: GDC-0575 analog)

发表于2023年11月7日由上海金畔生物科技有限公司

CHK1 inhibitor (Synonyms: GDC-0575 analog)

CHK1 inhibitor (GDC-0575 analog) 是 CHK1 的抑制剂。

CHK1 inhibitor Chemical Structure

CAS No. : 2097938-64-0

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1.

IC₅₀ & Target

CHK1

Clinical Trial

分子量

377.28

Formula

C₁₇H₂₁BrN₄O

CAS 号

2097938-64-0

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.

溶解性数据

In Vitro:

DMSO : 150 mg/mL (397.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6506 mL	13.2528 mL	26.5055 mL
5 mM	0.5301 mL	2.6506 mL	5.3011 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.63 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.63 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHK1-IN-2

发表于2023年11月7日由上海金畔生物科技有限公司

CHK1-IN-2

CHK1-IN-2 是细胞周期检测点激酶 (CHK1) 的抑制剂，其 IC₅₀ 为 6 nM。

CHK1-IN-2 Chemical Structure

CAS No. : 912367-45-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC₅₀ of 6 nM.

IC₅₀ & Target

Chk1

6 nM (IC₅₀)

体外研究
(In Vitro)

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC₅₀ of 6 nM, which is a potential cancer therapeutic that can be utilized for enhancing the efficacy of DNA damaging agents^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

366.48

Formula

C₂₀H₂₂N₄OS

CAS 号

912367-45-4

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.

参考文献

[1]. Yang B, et al. Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors. J Med Chem. 2018 Feb 8;61(3):1061-1073.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHK1-IN-4

发表于2023年8月25日由上海金畔生物科技有限公司

CHK1-IN-4

CHK1-IN-4 (化合物3) 是一种有效的关卡激酶 1 (chk1) 抑制剂，可有效抑制肿瘤细胞中 chk1 磷酸化。CHK1-IN-4 具有抗肿瘤活性。

CHK1-IN-4 Chemical Structure

CAS No. : 2120398-41-4

规格		是否有货
100 mg		询价
250 mg		询价
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生物活性

CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity^[1].

IC₅₀ & Target^[1]

Chk1

体内研究
(In Vivo)

CHK1-IN-4 (Compound 3) (40 mg/kg, IV, twice a week) alone enhances anti-tumor growth activity of CPT1 in the tumor model^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

444.29

Formula

C₁₈H₁₈BrN₇O₂

CAS 号

2120398-41-4

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.

参考文献

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHK1-IN-3

发表于2023年8月22日由上海金畔生物科技有限公司

CHK1-IN-3

CHK1-IN-3 是一种检测点激酶 (CHK1) 抑制剂，IC₅₀ 值为 0.4 nM。

CHK1-IN-3 Chemical Structure

CAS No. : 2097252-39-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC₅₀ of 0.4 nM^[1].

IC₅₀ & Target^[1]

Chk1

0.4 nM (IC₅₀)

体外研究
(In Vitro)

CHK1-IN-3 effectively inhibites the growth of malignant hematopathy cell lines especially Z-138 (IC50: 0.013 µM) and displays low affinity for hERG (IC50 > 40 µM)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CHK1-IN-3 significantly suppresses the tumor growth in Z-138 cell inoculated xenograft model as a single agent with body weight unaffected^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

405.46

Formula

C₂₀H₂₃N₉O

CAS 号

2097252-39-4

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.

参考文献

[1]. Tong L, et al. Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies. Eur J Med Chem. 2019 Jul 1;173:44-62.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

多肽定制[pS345]-Chk1 编码

发表于2023年7月27日由上海金畔生物科技有限公司

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	[pS345]-Chk1
编码
别名	[pS345]-Chk1
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	QGISF-pS-QPTC
序列（三字母缩写）	H-Gln-Gly-Ile-Ser-Phe-pSer-Gln-Pro-Thr-Cys-OH (trifluoroacetate salt)
基本描述	This amino acids 206 to 225 fragment corresponds to the phosphatase CDC25C, phosphorylated at position Ser217. This peptide can be used for checkpoint kinases CHK1 and CHK2 assays.
溶解度
分子量	1147.2
化学式
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference	Liu, Q. et al. Genes Dev. 14, 1448 (2000).
C端
N端
化学桥

多肽定制2 CDC25C, CHK1 and CHK2 Substrate, phospho 编码

发表于2023年7月17日由上海金畔生物科技有限公司

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	2 CDC25C, CHK1 and CHK2 Substrate, phospho
编码
别名	2 CDC25C, CHK1 and CHK2 Substrate, phospho
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	KKKVSRSGLYR-pS-PSMPENLNRPR-NH2
序列（三字母缩写）	H-Lys-Lys-Lys-Val-Ser-Arg-Ser-Gly-Leu-Tyr-Arg-pSer-Pro-Ser-Met-Pro-Glu-Asn-Leu-Asn-Arg-Pro-Arg-NH2?(trifluoroacetate salt)
基本描述	The native peptide ARKRERTYSFGHHA (29944-1) is a synthetic substrate for AKT/PKB/Rac-protein kinases. Phophorylation is at the Ser site (Km = 3.9 碌M). It also competitively inhibits histone H2B phosphorylation (Ki = 12 碌M) by AKT.
溶解度
分子量	2780.2
化学式
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference	Jiang, X. et al. Mol. Canc. Ther. 3: 1221 (2004) O?Neill, T. et al. J. Biol. Chem. 277, 16102 (2002 Davies, S. et al. Biochem. J. 351, 95 (2000) Oh, H. et al. Proc. Natl. Acad. Sci. USA 100, 5378 (2003).
C端
N端
化学桥

赛默飞Alfa aesar官网

赛默飞Acros试剂中国官网 Alfa aesar阿法埃莎中国代理商

标签归档：chk

BML-277(Synonyms: Chk2 Inhibitor II)

BML-277 相关产品

•相关化合物库:

Chk1-IN-5

Chk1-IN-5

Chk1-IN-5

Chk1-IN-6

Chk1-IN-6

Chk1-IN-6

CHK1 inhibitor(Synonyms: GDC-0575 analog)

CHK1-IN-2

CHK1-IN-4

CHK1-IN-3

多肽定制[pS345]-Chk1 编码

多肽定制2 CDC25C, CHK1 and CHK2 Substrate, phospho 编码