标签归档：pkc

O-Desmethyl Midostaurin-d5(Synonyms: CGP62221-d5; O-Desmethyl PKC412-d5)

发表于由

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。

O-Desmethyl Midostaurin-d5 (Synonyms: CGP62221-d5; O-Desmethyl PKC412-d5)

O-Desmethyl PKC412-d5 (CGP62221-d5) 是 O-Desmethyl PKC412 的氘代物。O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) 是 Midostaurin (HY-10230) 的活性代谢物，通过细胞色素 P450 肝酶代谢产生，可以作为 Midostaurin 在体内代谢的指标之一。

O-Desmethyl Midostaurin-d5(Synonyms: CGP62221-d5; O-Desmethyl PKC412-d5)

O-Desmethyl Midostaurin-d5 Chemical Structure

规格 价格 是否有货
1 mg ￥10500 询问价格 & 货期

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生物活性

O-Desmethyl PKC412-d5 (CGP62221-d5) is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism[1].

IC50 & Target

IC50: active metabolite of Midostaurin[1]
分子量

561.64

Formula

C34H23D5N4O4
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]. Levis M, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors. Blood. 2006 Nov 15;108(10):3477-83.

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PS315

发表于由

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。

PS315 

PS315 是 PS48 (HY-15967) 的衍生物，是一种变构性 PKC 抑制剂，可以与 aPKC 的 PIF 口袋结合并诱导活性位点残基 Lys111 置换。PS315 抑制 PKCζ (IC50=10 μM) 和 PKCη (IC50=30 μM) 的全长和催化结构域构建体。PS315 具有抗癌活性。

PS315

PS315 Chemical Structure

CAS No. : 1221964-50-6

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250 mg   询价  
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生物活性

PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity[1].

IC50 & Target[1]

PKCζ

10 μM (IC50)

PKCη

30 μM (IC50)

体外研究
(In Vitro)

Preincubation of U937 cells with 5 μM PS315 inhibits TNF-α induced NF-κB activation by 74%, whereas complete inhibition is observed with 10 μM PS315[1].
The small allosteric inhibitor PS315 and the N-terminal region of aPKC both act directly on the PIF-pocket on-off switch. PS315, binding at the PIF-pocket, induces a displacement of the active site residue Lys111, thereby inhibiting the activity of aPKCs by allosterically affecting the catalytic mechanism of the kinase[1].

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

362.85

Formula

C23H19ClO2
CAS 号

1221964-50-6
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]. Zhang H, et al. Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound. Chem Biol. 2014 Jun 19;21(6):754-65.

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

PS315

发表于由

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。

PS315 

PS315 是 PS48 (HY-15967) 的衍生物，是一种变构性 PKC 抑制剂，可以与 aPKC 的 PIF 口袋结合并诱导活性位点残基 Lys111 置换。PS315 抑制 PKCζ (IC50=10 μM) 和 PKCη (IC50=30 μM) 的全长和催化结构域构建体。PS315 具有抗癌活性。

PS315

PS315 Chemical Structure

CAS No. : 1221964-50-6

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

PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity[1].

IC50 & Target[1]

PKCζ

10 μM (IC50)

PKCη

30 μM (IC50)

体外研究
(In Vitro)

Preincubation of U937 cells with 5 μM PS315 inhibits TNF-α induced NF-κB activation by 74%, whereas complete inhibition is observed with 10 μM PS315[1].
The small allosteric inhibitor PS315 and the N-terminal region of aPKC both act directly on the PIF-pocket on-off switch. PS315, binding at the PIF-pocket, induces a displacement of the active site residue Lys111, thereby inhibiting the activity of aPKCs by allosterically affecting the catalytic mechanism of the kinase[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

362.85

Formula

C23H19ClO2
CAS 号

1221964-50-6
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]. Zhang H, et al. Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound. Chem Biol. 2014 Jun 19;21(6):754-65.

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

PS315

发表于由

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。

PS315 

PS315 是 PS48 (HY-15967) 的衍生物，是一种变构性 PKC 抑制剂，可以与 aPKC 的 PIF 口袋结合并诱导活性位点残基 Lys111 置换。PS315 抑制 PKCζ (IC50=10 μM) 和 PKCη (IC50=30 μM) 的全长和催化结构域构建体。PS315 具有抗癌活性。

PS315

PS315 Chemical Structure

CAS No. : 1221964-50-6

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

PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity[1].

IC50 & Target[1]

PKCζ

10 μM (IC50)

PKCη

30 μM (IC50)

体外研究
(In Vitro)

Preincubation of U937 cells with 5 μM PS315 inhibits TNF-α induced NF-κB activation by 74%, whereas complete inhibition is observed with 10 μM PS315[1].
The small allosteric inhibitor PS315 and the N-terminal region of aPKC both act directly on the PIF-pocket on-off switch. PS315, binding at the PIF-pocket, induces a displacement of the active site residue Lys111, thereby inhibiting the activity of aPKCs by allosterically affecting the catalytic mechanism of the kinase[1].

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

362.85

Formula

C23H19ClO2
CAS 号

1221964-50-6
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]. Zhang H, et al. Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound. Chem Biol. 2014 Jun 19;21(6):754-65.

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

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

发表于由

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。

Mezerein (Synonyms: 密执毒素；欧瑞香脂；)

Mezerein 是一种 PKC 激活剂，具有抗白血病特性。 Mezerein 抑制表达 PKC alpha (IC50=1190 nM)、PKC beta1 (IC50=908 nM) 和 PKC delta (IC50=141 nM) 的酵母生长，但不抑制表达 PKC 的酵母生长。

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

Mezerein Chemical Structure

CAS No. : 34807-41-5

规格 是否有货
5 mg 询价
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25 mg 询价

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生物活性

Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC[1][2].

体外研究
(In Vitro)

Mezerein is an antileukemic principle isolated from Daphne mezereum L[2].
Mezerein (50 ng/mL; 72 hours) potently inhibit tumorigenic murine macrophage cell line M5076 cellular proliferation[3].

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

Cell Proliferation Assay[3]

Cell Line: M5076 cells
Concentration: 50 ng/mL
Incubation Time: 72 hours
Result: Inhibited cellular proliferation (by greater than 90%).

体内研究
(In Vivo)

Mezerein exhibits antileukemic activity against the P-388 lymphocytic leukemia in mice. Mezerein (50 μg/kg) shows significant inhibitory activity against the P-388 and L-1210 leukemias in mice[2].

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

654.70

Formula

C38H38O10
CAS 号

34807-41-5
中文名称

密执毒素；欧瑞香脂；
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]. L Saraiva, et al. Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta. Planta Med. 2001 Dec;67(9):787-90.

    [2]. S M Kupchan,et al.Mezerein: antileukemic principle isolated from Daphne mezereum L. Science. 1975 Feb 21;187(4177):652-3.

    [3]. N T Goode, et al. Protein kinase C-induced stimulation or inhibition of cellular proliferation in a murine macrophage tumor cell line. Cancer Res. 1990 Mar 15;50(6):1828-33.

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

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

发表于由

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。

Mezerein (Synonyms: 密执毒素；欧瑞香脂；)

Mezerein 是一种 PKC 激活剂，具有抗白血病特性。 Mezerein 抑制表达 PKC alpha (IC50=1190 nM)、PKC beta1 (IC50=908 nM) 和 PKC delta (IC50=141 nM) 的酵母生长，但不抑制表达 PKC 的酵母生长。

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

Mezerein Chemical Structure

CAS No. : 34807-41-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC[1][2].

体外研究
(In Vitro)

Mezerein is an antileukemic principle isolated from Daphne mezereum L[2].
Mezerein (50 ng/mL; 72 hours) potently inhibit tumorigenic murine macrophage cell line M5076 cellular proliferation[3].

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

Cell Proliferation Assay[3]

Cell Line: M5076 cells
Concentration: 50 ng/mL
Incubation Time: 72 hours
Result: Inhibited cellular proliferation (by greater than 90%).

体内研究
(In Vivo)

Mezerein exhibits antileukemic activity against the P-388 lymphocytic leukemia in mice. Mezerein (50 μg/kg) shows significant inhibitory activity against the P-388 and L-1210 leukemias in mice[2].

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

654.70

Formula

C38H38O10
CAS 号

34807-41-5
中文名称

密执毒素；欧瑞香脂；
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]. L Saraiva, et al. Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta. Planta Med. 2001 Dec;67(9):787-90.

    [2]. S M Kupchan,et al.Mezerein: antileukemic principle isolated from Daphne mezereum L. Science. 1975 Feb 21;187(4177):652-3.

    [3]. N T Goode, et al. Protein kinase C-induced stimulation or inhibition of cellular proliferation in a murine macrophage tumor cell line. Cancer Res. 1990 Mar 15;50(6):1828-33.

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

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

发表于由

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。

Mezerein (Synonyms: 密执毒素；欧瑞香脂；)

Mezerein 是一种 PKC 激活剂，具有抗白血病特性。 Mezerein 抑制表达 PKC alpha (IC50=1190 nM)、PKC beta1 (IC50=908 nM) 和 PKC delta (IC50=141 nM) 的酵母生长，但不抑制表达 PKC 的酵母生长。

Mezerein(Synonyms: 密执毒素；欧瑞香脂；)

Mezerein Chemical Structure

CAS No. : 34807-41-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC[1][2].

体外研究
(In Vitro)

Mezerein is an antileukemic principle isolated from Daphne mezereum L[2].
Mezerein (50 ng/mL; 72 hours) potently inhibit tumorigenic murine macrophage cell line M5076 cellular proliferation[3].

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 Proliferation Assay[3]

Cell Line: M5076 cells
Concentration: 50 ng/mL
Incubation Time: 72 hours
Result: Inhibited cellular proliferation (by greater than 90%).

体内研究
(In Vivo)

Mezerein exhibits antileukemic activity against the P-388 lymphocytic leukemia in mice. Mezerein (50 μg/kg) shows significant inhibitory activity against the P-388 and L-1210 leukemias in mice[2].

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

654.70

Formula

C38H38O10
CAS 号

34807-41-5
中文名称

密执毒素；欧瑞香脂；
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]. L Saraiva, et al. Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta. Planta Med. 2001 Dec;67(9):787-90.

    [2]. S M Kupchan,et al.Mezerein: antileukemic principle isolated from Daphne mezereum L. Science. 1975 Feb 21;187(4177):652-3.

    [3]. N T Goode, et al. Protein kinase C-induced stimulation or inhibition of cellular proliferation in a murine macrophage tumor cell line. Cancer Res. 1990 Mar 15;50(6):1828-33.

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

PKCiota-IN-2

发表于由

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。

PKCiota-IN-2 

PKCiota-IN-2 是一种有效的 PKCiota (PKC-ι) 抑制剂，IC50 为 2.8 nM。PKCiota-IN-2 还抑制 PKC-α 和 PKC-ε，IC50 分别为 71 nM 和 350 nM。

PKCiota-IN-2

PKCiota-IN-2 Chemical Structure

CAS No. : 2230055-52-2

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

PKCiota-IN-2 is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively[1].

IC50 & Target[1]

PKCι

2.8 nM (IC50)

PKCα

71 nM (IC50)

PKCε

350 nM (IC50)

分子量

395.46

Formula

C24H21N5O
CAS 号

2230055-52-2
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]. Jacek Kwiatkowski, et al. Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors. J Med Chem. 2018 May 24;61(10):4386-4396.

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多肽定制PKC-epsilon pseudosubstrate derived peptide 编码 [120253-69-2]

发表于由

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 PKC-epsilon pseudosubstrate derived peptide
编码 [120253-69-2]
别名 PKC-epsilon pseudosubstrate derived peptide
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） ERMRPRKRQGSVRRRV
序列（三字母缩写） Glu-Arg-Met-Arg-Pro-Arg-Lys-Arg-Gln-Gly-Ser-Val-Arg-Arg-Arg-Val
基本描述
溶解度
分子量 2067.47
化学式 C83H155N39O21S
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents PKC-epsilon pseudosubstrate derived peptide 编码 [120253-69-2]
Figures PKC-epsilon pseudosubstrate derived peptide 编码 [120253-69-2]
Reference
C端
N端
化学桥

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

发表于由

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。

(-)-Indolactam V-d8 (Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 (Indolactam V-d8) 是 (-)-Indolactam V 的氘代物。(-)-Indolactam V 是 PKC 的激活剂，对 η-CRD2 (PKCη 代替肽)，γ-CRD2 (PKCγ 代替肽) 的 Ki 值分别为 3.36 nM 和 1.03 μM，对 PKC C1A 和 C1B 结构域的 Kd 值分别为 5.5 nM (η-C1B)，7.7 nM (ε-C1

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 Chemical Structure

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

(-)-Indolactam V-d8 (Indolactam V-d8) is the deuterium labeled (-)-Indolactam V. (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

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

309.43

Formula

C17H15D8N3O2
中文名称

吲哚内酰胺 V d8
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]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

    [3]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

    [4]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

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

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

发表于由

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。

(-)-Indolactam V-d8 (Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 (Indolactam V-d8) 是 (-)-Indolactam V 的氘代物。(-)-Indolactam V 是 PKC 的激活剂，对 η-CRD2 (PKCη 代替肽)，γ-CRD2 (PKCγ 代替肽) 的 Ki 值分别为 3.36 nM 和 1.03 μM，对 PKC C1A 和 C1B 结构域的 Kd 值分别为 5.5 nM (η-C1B)，7.7 nM (ε-C1

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 Chemical Structure

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

(-)-Indolactam V-d8 (Indolactam V-d8) is the deuterium labeled (-)-Indolactam V. (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

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

309.43

Formula

C17H15D8N3O2
中文名称

吲哚内酰胺 V d8
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]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

    [3]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

    [4]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

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

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

发表于由

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。

(-)-Indolactam V-d8 (Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 (Indolactam V-d8) 是 (-)-Indolactam V 的氘代物。(-)-Indolactam V 是 PKC 的激活剂，对 η-CRD2 (PKCη 代替肽)，γ-CRD2 (PKCγ 代替肽) 的 Ki 值分别为 3.36 nM 和 1.03 μM，对 PKC C1A 和 C1B 结构域的 Kd 值分别为 5.5 nM (η-C1B)，7.7 nM (ε-C1

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 Chemical Structure

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

(-)-Indolactam V-d8 (Indolactam V-d8) is the deuterium labeled (-)-Indolactam V. (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

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

309.43

Formula

C17H15D8N3O2
中文名称

吲哚内酰胺 V d8
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]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

    [3]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

    [4]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

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