PERK-IN-2

发表于2024年1月20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。

PERK-IN-2

PERK-IN-2 是一种高效的 PERK 抑制剂，其 IC₅₀ 值为 0.2 nM。

PERK-IN-2 Chemical Structure

CAS No. : 1337531-83-5

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生物活性

PERK-IN-2 is a potent PERK inhibitor with an IC₅₀ of 0.2 nM^[1].

IC₅₀ & Target

IC50: 0.2 nM (PERK)^[1]

体外研究
(In Vitro)

PERK-IN-2 (0.03-0.3 μM; 2 hours) inhibits PERK autophosphorylation in A459 cells with IC₅₀ value ranging from 0.03−0.1 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	A459 cells
Concentration:	0.03 μM, 0.1 μM, 0.3 μM
Incubation Time:	2 hours
Result:	Inhibited PERK autophosphorylation in A459 cells.

分子量

437.42

Formula

C₂₃H₁₈F₃N₅O

CAS 号

1337531-83-5

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]. Axten JM , et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.

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PERK-IN-2

发表于2024年1月20日由上海金畔生物科技有限公司

PERK-IN-2

PERK-IN-2 是一种高效的 PERK 抑制剂，其 IC₅₀ 值为 0.2 nM。

PERK-IN-2 Chemical Structure

CAS No. : 1337531-83-5

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250 mg		询价
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生物活性

PERK-IN-2 is a potent PERK inhibitor with an IC₅₀ of 0.2 nM^[1].

IC₅₀ & Target

IC50: 0.2 nM (PERK)^[1]

体外研究
(In Vitro)

PERK-IN-2 (0.03-0.3 μM; 2 hours) inhibits PERK autophosphorylation in A459 cells with IC₅₀ value ranging from 0.03−0.1 μM^[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 Viability Assay^[1]

Cell Line:	A459 cells
Concentration:	0.03 μM, 0.1 μM, 0.3 μM
Incubation Time:	2 hours
Result:	Inhibited PERK autophosphorylation in A459 cells.

分子量

437.42

Formula

C₂₃H₁₈F₃N₅O

CAS 号

1337531-83-5

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]. Axten JM , et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.

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

PERK-IN-2

发表于2024年1月20日由上海金畔生物科技有限公司

PERK-IN-2

PERK-IN-2 是一种高效的 PERK 抑制剂，其 IC₅₀ 值为 0.2 nM。

PERK-IN-2 Chemical Structure

CAS No. : 1337531-83-5

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

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生物活性

PERK-IN-2 is a potent PERK inhibitor with an IC₅₀ of 0.2 nM^[1].

IC₅₀ & Target

IC50: 0.2 nM (PERK)^[1]

体外研究
(In Vitro)

PERK-IN-2 (0.03-0.3 μM; 2 hours) inhibits PERK autophosphorylation in A459 cells with IC₅₀ value ranging from 0.03−0.1 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	A459 cells
Concentration:	0.03 μM, 0.1 μM, 0.3 μM
Incubation Time:	2 hours
Result:	Inhibited PERK autophosphorylation in A459 cells.

分子量

437.42

Formula

C₂₃H₁₈F₃N₅O

CAS 号

1337531-83-5

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]. Axten JM , et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.

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

PERK-IN-3

发表于2024年1月19日由上海金畔生物科技有限公司

PERK-IN-3

PERK-IN-3 是一种高效的 PERK 抑制剂，其 IC₅₀ 值为 7.4 nM。

PERK-IN-3 Chemical Structure

CAS No. : 1337532-08-7

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生物活性	PERK-IN-3 is a potent PERK inhibitor with an IC₅₀ of 7.4 nM^[1].
IC₅₀ & Target	IC50: 7.4 nM (PERK)^[1]
分子量	406.38
Formula	C₂₂H₁₆F₂N₄O₂
CAS 号	1337532-08-7
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.
参考文献	[1]. Axten JM , et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.

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

PERK-IN-3

发表于2024年1月18日由上海金畔生物科技有限公司

PERK-IN-3

PERK-IN-3 是一种高效的 PERK 抑制剂，其 IC₅₀ 值为 7.4 nM。

PERK-IN-3 Chemical Structure

CAS No. : 1337532-08-7

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生物活性	PERK-IN-3 is a potent PERK inhibitor with an IC₅₀ of 7.4 nM^[1].
IC₅₀ & Target	IC50: 7.4 nM (PERK)^[1]
分子量	406.38
Formula	C₂₂H₁₆F₂N₄O₂
CAS 号	1337532-08-7
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.
参考文献	[1]. Axten JM , et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.

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

PERK-IN-4-d3

发表于2023年12月19日由上海金畔生物科技有限公司

PERK-IN-4-d3

PERK-IN-4-d3 是 PERK-IN-4 的氘代物。PERK-IN-4 是一种有效的选择性PERK抑制剂，IC ₅₀ 值为 0.3 nM。PERK 响应与多种疾病状态有关的内质网应激而被激活。

PERK-IN-4-d3 Chemical Structure

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生物活性	PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	472.45
Formula	C₂₄H₁₆D₃F₄N₅O
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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PERK-IN-4-d3

发表于2023年12月19日由上海金畔生物科技有限公司

PERK-IN-4-d3

PERK-IN-4-d3 Chemical Structure

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生物活性	PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	472.45
Formula	C₂₄H₁₆D₃F₄N₅O
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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

PERK-IN-4-d3

发表于2023年12月19日由上海金畔生物科技有限公司

PERK-IN-4-d3

PERK-IN-4-d3 Chemical Structure

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生物活性	PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[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	472.45
Formula	C₂₄H₁₆D₃F₄N₅O
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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

PERK-IN-4

发表于2023年12月13日由上海金畔生物科技有限公司

PERK-IN-4

PERK-IN-4 是一种有效的选择性PERK抑制剂，IC ₅₀ 值为 0.3 nM。PERK 响应与多种疾病状态有关的内质网应激而被激活。

PERK-IN-4 Chemical Structure

CAS No. : 1337531-89-1

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生物活性	PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
IC₅₀ & Target	IC50: 0.3 nM (PERK)^[1]
分子量	469.43
Formula	C₂₄H₁₉F₄N₅O
CAS 号	1337531-89-1
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]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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

PERK-IN-4

发表于2023年12月13日由上海金畔生物科技有限公司

PERK-IN-4

PERK-IN-4 是一种有效的选择性PERK抑制剂，IC ₅₀ 值为 0.3 nM。PERK 响应与多种疾病状态有关的内质网应激而被激活。

PERK-IN-4 Chemical Structure

CAS No. : 1337531-89-1

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100 mg		询价
250 mg		询价
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生物活性	PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
IC₅₀ & Target	IC50: 0.3 nM (PERK)^[1]
分子量	469.43
Formula	C₂₄H₁₉F₄N₅O
CAS 号	1337531-89-1
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]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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

PERK-IN-4

发表于2023年12月13日由上海金畔生物科技有限公司

PERK-IN-4

PERK-IN-4 是一种有效的选择性PERK抑制剂，IC ₅₀ 值为 0.3 nM。PERK 响应与多种疾病状态有关的内质网应激而被激活。

PERK-IN-4 Chemical Structure

CAS No. : 1337531-89-1

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生物活性	PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC ₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states^[1].
IC₅₀ & Target	IC50: 0.3 nM (PERK)^[1]
分子量	469.43
Formula	C₂₄H₁₉F₄N₅O
CAS 号	1337531-89-1
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]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

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AMG PERK 44

发表于2023年8月4日由上海金畔生物科技有限公司

AMG PERK 44 纯度: 99.17%

AMG PERK 44 是一种口服有效的，高选择性的 PERK 抑制剂，IC₅₀ 为 6 nM。AMG PERK 44 对 PERK 的选择性分别是 GCN2 (IC₅₀=7300 nM) 和 B-Raf (IC₅₀ >1000 nM) 的 1000 倍和 160 倍。AMG PERK 44 可以诱导自噬 (autophagy)。

AMG PERK 44 Chemical Structure

CAS No. : 1883548-84-2

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Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
50 mg	￥9500	In-stock
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AMG PERK 44 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Endoplasmic Reticulum Stress Compound Library
Targeted Diversity Library

生物活性

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC₅₀ of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC₅₀=7300 nM) and B-Raf (IC₅₀ >1000 nM), respectively. AMG PERK 44 induces autophagy^[1]^[2].

IC₅₀ & Target

IC50: 6 nM (PERK)^[1]

体外研究
(In Vitro)

AMG PERK 44 has an IC₅₀ of 84 nM for cell pPERK^[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)

AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (ED₅₀=3 mg/kg; ED₉₀=60 mg/kg at the 4 hours time point), and >50% target coverage is maintained for 24 h in a time course PD assay when dosed at 100 mg/kg po^[1].
AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h•kg, a V_ss of 3.6 L/kg and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice^[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.

Animal Model:	Four- to six-week old naive athymic nude mice^[1]
Dosage:	3, 10, 30, 100 mg/kg
Administration:	Orally
Result:	Robustly inhibited PERK autophosphorylation in this assay (ED₅₀=3 mg/kg; ED₉₀=60 mg/kg at the 4 hours time point).

Animal Model:	Sprague-Dawley rats and male CD-1 mice^[1]
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv
Result:	Had a CL of 1.6 L/h•kg, a V_ss of 3.6 L/kg and a MRT of 2.3 hours.

分子量

561.07

Formula

C₃₄H₂₉ClN₄O₂

CAS 号

1883548-84-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 25 mg/mL (44.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7823 mL	8.9115 mL	17.8231 mL
5 mM	0.3565 mL	1.7823 mL	3.5646 mL
10 mM	0.1782 mL	0.8912 mL	1.7823 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (3.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.71 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.71 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.71 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 20.8 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]. Smith AL, et al. Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem. 2015 Feb 12;58(3):1426-41.

[2]. Roest G, et al. The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells. 2018 Nov 30;7(12). pii: E239.

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

PERK-IN-5

发表于2023年5月11日由上海金畔生物科技有限公司

PERK-IN-5

PERK-IN-5 是一种高效、高选择性且口服生物可利用的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂，PERK 与 p-eIF2α 的 IC₅₀ 为 2 nM 和 9 nM。PERK-IN-5 在 786-O 肾细胞癌异种移植瘤模型中，能显著抑制肿瘤生长。

PERK-IN-5 Chemical Structure

CAS No. : 2616821-91-9

规格	价格	是否有货
5 mg	￥7500	询问价格 & 货期
10 mg	￥12000	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC₅₀s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model^[1].

IC₅₀ & Target

IC₅₀: 2 nM (PERK), 9 nM (p-eIF2α)^[1]

体外研究
(In Vitro)

PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives^[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)

PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with C_max of 3353 ng/mL, AUC_0-last of 5153 h*ng/mL, and bioavailability of 70%^[1].
PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition^[1].

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

Animal Model:	Female CD1 mice^[1] (Pharmacokinetics)
Dosage:	3, 10, 30 and 100 mg/kg
Administration:	p.o.; 0.25-24 hours
Result:	Showed robust pharmacokinetics with C_max of 3353 ng/mL, AUC_0-last of 5153 h*ng/mL, and bioavailability of 70%.

Animal Model:	BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells)^[1]
Dosage:	3 or 10 mg/kg
Administration:	p.o.; twice daily, for 28 days
Result:	Showed statistically significant tumor growth inhibition.

分子量

468.50

Formula

C₂₅H₂₆F₂N₄O₃

CAS 号

2616821-91-9

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]. Calvo V, et al. Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Bioorg Med Chem Lett. 2021;43:128058.

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标签归档：perk

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AMG PERK 44

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