PRMT1-IN-1

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。

PRMT1-IN-1 

PRMT1-IN-1 是一种 PRMT1 抑制剂。

PRMT1-IN-1

PRMT1-IN-1 Chemical Structure

CAS No. : 1025948-98-4

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生物活性

PRMT1-IN-1 is a PRMT1 inhibitor.

分子量

820.70

Formula

C20H7Br6NO5

CAS 号

1025948-98-4

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.

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PROTAC CDK9 degrader-4

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。

PROTAC CDK9 degrader-4 

PROTAC CDK9 degrader-4 是一种高效、靶向转录调控的 CDK9 降解物。

PROTAC CDK9 degrader-4

PROTAC CDK9 degrader-4 Chemical Structure

CAS No. : 2411021-01-5

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生物活性

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

分子量

792.97

Formula

C43H56N10O5

CAS 号

2411021-01-5

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]. Wei D, et al. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J Med Chem. 2021 Oct 14;64(19):14822-14847.

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BPR1R024

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。

BPR1R024 

BPR1R024 是一种口服活性和选择性的 CSF1R 抑制剂(IC50 = 0.53 nM)。

BPR1R024

BPR1R024 Chemical Structure

CAS No. : 2503015-75-4

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生物活性

BPR1R024 is an orally active and selective CSF1R inhibitor (IC50 = 0.53 nM).

分子量

482.46

Formula

C24H21F3N6O2

CAS 号

2503015-75-4

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]. Lee KH, et al. Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model. J Med Chem. 2021 Oct 14;64(19):14477-14497.

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Okadaic acid ammonium salt(Synonyms: 冈田酸铵盐)

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。

Okadaic acid ammonium salt (Synonyms: 冈田酸铵盐)

Okadaic acid ammonium salt 是一种海洋毒素,是蛋白质磷酸酶 (PP) 的抑制剂,包括 PP1 (IC50=15-50 nM)、PP2A (IC50=0.1-0.3 nM)、PP3 (IC50=3.7-4 nM)、PP4 (IC50=0.1 nM) 和 PP5 (IC50=3.5 nM),其中对 PP2A 的亲和力最显著,但不抑制 PP2C。Okadaic acid ammonium salt 通过抑制 PP 增加了多种蛋白的磷酸化,并具有肿瘤启动子的作用。Okadaic acid ammonium salt 诱导 tau 蛋白磷酸化。

Okadaic acid ammonium salt(Synonyms: 冈田酸铵盐)

Okadaic acid ammonium salt Chemical Structure

CAS No. : 175522-42-6

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Okadaic acid ammonium salt 的其他形式现货产品:

Okadaic acid

生物活性

Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation[1][2].

IC50 & Target[1]

PP1

15-50 nM (IC50)

PP2A

0.1-0.3 nM (IC50)

PP3

3.7-4 nM (IC50)

PP4

0.1 nM (IC50)

PP5

3.5 nM (IC50)

PP2B

~4000 nM (IC50)

PP7

>1000 nM (IC50)

体外研究
(In Vitro)

Okadaic acid ammonium salt (0-100 nM; 24 h or 48 h) inhibits the proliferation of AGS, MNK-45, Caco 2 cells[3].
Okadaic acid (10 nM, 8 hours) ammonium salt increases Drp1 phosphorylation and mitochondrial fission in rat cortical neurons[4].

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: AGS, MNK-45 and Caco 2 cell lines
Concentration: 0-100 nM
Incubation Time: 24 h or 48 h
Result: Inhibited the proliferation of AGS, MNK-45, Caco 2 cells.

体内研究
(In Vivo)

Okadaic acid ammonium salt (100 μM; injected unilaterally to the lateral amygdala) induces Tau phosphorylation and protein aggregation in anatomically distinct brain regions 24 h post-injection[5].

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

Animal Model: Female wild-type C57BL/6 mice (6 to 8 months)[5]
Dosage: 100 μM
Administration: Injected unilaterally to the lateral amygdala
Result: Induced Tau phosphorylation and protein aggregation in anatomically distinct brain regions 24 h post-injection.

分子量

822.03

Formula

C44H71NO13

CAS 号

175522-42-6

中文名称

冈田酸铵盐

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]. Kleppe R, et al. Cell Death Inducing Microbial Protein Phosphatase Inhibitors–Mechanisms of Action. Mar Drugs. 2015 Oct 22;13(10):6505-20.

    [2]. Valdiglesias V, et al. Okadaic acid: more than a diarrheic toxin. Mar Drugs. 2013 Oct 31;11(11):4328-49.

    [3]. del Campo M, et al. Okadaic acid toxin at sublethal dose produced cell proliferation in gastric and colon epithelial cell lines. Mar Drugs. 2013;11(12):4751-4760.

    [4]. Cho MH, et al. Increased phosphorylation of dynamin-related protein 1 and mitochondrial fission in okadaic acid-treated neurons. Brain Res. 2012 May 15;1454:100-10.

    [5]. Baker S, et al. A local insult of okadaic acid in wild-type mice induces tau phosphorylation and protein aggregation in anatomically distinct brain regions. Acta Neuropathol Commun. 2016;4:32.

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RAD51-IN-4

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。

RAD51-IN-4 

RAD51-IN-4 是一种有效的 RAD51 抑制剂。RAD51 是一种真核生物基因。RAD51-IN-4 具有研究线粒体缺陷病症的潜力 (摘自专利 WO2019014315A1,化合物 R12)。

RAD51-IN-4

RAD51-IN-4 Chemical Structure

CAS No. : 2267336-26-3

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生物活性

RAD51-IN-4 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-4 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2019014315A1, compound R12)[1].

分子量

639.76

Formula

C31H34FN5O5S2

CAS 号

2267336-26-3

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]. Alfredo C. Castro, et al. Rad51 inhibitors. Patent WO2019014315A1.

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PROTAC CDK9 ligand-1

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。

PROTAC CDK9 ligand-1 

PROTAC CDK9 ligand-1 是一种可用于合成 PROTAC 的 CDK9 配体。

PROTAC CDK9 ligand-1

PROTAC CDK9 ligand-1 Chemical Structure

CAS No. : 2411021-95-7

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生物活性

PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.

分子量

368.48

Formula

C20H28N6O

CAS 号

2411021-95-7

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]. Wei D, et al. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J Med Chem. 2021 Oct 14;64(19):14822-14847.

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Cathepsin L-IN-2(Synonyms: Z-Phe-Phe-FMK)

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。

Cathepsin L-IN-2 (Synonyms: Z-Phe-Phe-FMK)

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) 是一种有效且不可逆的组织蛋白酶 L (cathepsin L) 和组织蛋白酶 B (cathepsin B) 抑制剂。

Cathepsin L-IN-2(Synonyms: Z-Phe-Phe-FMK)

Cathepsin L-IN-2 Chemical Structure

CAS No. : 108005-94-3

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生物活性

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor[1][2].

分子量

462.51

Formula

C27H27FN2O4

CAS 号

108005-94-3

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]. Jonathan Frew, et al. Premature termination codon readthrough upregulates progranulin expression and improves lysosomal function in preclinical models of GRN deficiency. Mol Neurodegener. 2020 Mar 16;15(1):21.

    [2]. Kirsi Ravanko, et al. Cysteine cathepsins are central contributors of invasion by cultured adenosylmethionine decarboxylase-transformed rodent fibroblasts. Cancer Res. 2004 Dec 15;64(24):8831-8.

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Anticancer agent 63

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。

Anticancer agent 63 

Anticancer agent 63 (化合物 3h) 对SW480、HeLa、A549和MCF-7等不同癌细胞株的活性均有明显的降低作用,在24 h 时其 IC50 值分别为 4.9、11.5、9.4和3.4 μM。Anticancer agent 63 通过下调 Bcl-2 表达、上调 IL-2 和 Caspase-3 表达诱导 MCF-7 细胞凋亡。Anticancer agent 63 还具有抗氧化活性。

Anticancer agent 63

Anticancer agent 63 Chemical Structure

CAS No. : 2529657-32-5

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生物活性

Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity[1].

IC50 & Target

Caspase-3

 

Bcl-2

 

分子量

394.33

Formula

C17H24F3NOSe

CAS 号

2529657-32-5

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]. He X, et al. Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF3) derivatives as potential anticancer agents. Eur J Med Chem. 2020 Dec 15;208:112864.

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Dihydrochlamydocin

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。

Dihydrochlamydocin 

Dihydrochlamydocin 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂。Dihydrochlamydocin 强烈抑制肥大细胞瘤的细胞活性。

Dihydrochlamydocin

Dihydrochlamydocin Chemical Structure

CAS No. : 52574-64-8

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生物活性

Dihydrochlamydocin is a histone deacetylases (HDAC) inhibitor. Dihydrochlamydocin shows strong cytostatic activity towards mastocytoma cells[1].

IC50 & Target

HDAC[1]

分子量

528.64

Formula

C28H40N4O6

CAS 号

52574-64-8

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]. Degenkolb T, et al. Metabolites from nematophagous fungi and nematicidal natural products from fungi as an alternative for biological control. Part I: metabolites from nematophagous ascomycetes. Appl Microbiol Biotechnol. 2016;100(9):3799-3812.

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Thalidomide-4-O-C10-COOH

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。

Thalidomide-4-O-C10-COOH  纯度: 98.86%

Thalidomide-4-O-C10-COOH 是一种 E3 连接酶配体-连接子共轭物,可用于合成 PROTAC。

Thalidomide-4-O-C10-COOH

Thalidomide-4-O-C10-COOH Chemical Structure

CAS No. : 2379870-45-6

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生物活性

Thalidomide-4-O-C10-COOH is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.

分子量

458.50

Formula

C24H30N2O7

CAS 号

2379870-45-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

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

参考文献
  • [1]. Powell CE, et al. Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC Med Chem. 2021 Jul 6;12(8):1381-1390.

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L-threo-PPMP

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。

L-threo-PPMP 

L-threo-PPMP 是一种 GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) 抑制剂。L-threo-PPMP 抑制鞘糖脂生物合成并诱导细胞凋亡。L-threo-PPMP 具有抗癌活性。

L-threo-PPMP

L-threo-PPMP Chemical Structure

CAS No. : 207278-87-3

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生物活性

L-threo-PPMP is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP has anti-cancer activity[1].

体外研究
(In Vitro)

L-threo-PPMP (0.5-20 μM) induces apoptosis in carcinoma (Colo-205; SKBR3) cells after 6 h and damaging DNA between 24 and 48 h after treatment[1].
L-threo-PPMP (1-16 μM; 48 hours) includes Caspase-3 activation in breast cancer SKBR3 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.

分子量

474.72

Formula

C29H50N2O3

CAS 号

207278-87-3

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]. Subhash Basu, et al. Apoptosis of human carcinoma cells in the presence of inhibitors of glycosphingolipid biosynthesis: I. Treatment of Colo-205 and SKBR3 cells with isomers of PDMP and PPMP. Glycoconj J. 2004;20(3):157-68.

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PROTAC CDK9 degrader-4

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。

PROTAC CDK9 degrader-4 

PROTAC CDK9 degrader-4 是一种高效、靶向转录调控的 CDK9 降解物。

PROTAC CDK9 degrader-4

PROTAC CDK9 degrader-4 Chemical Structure

CAS No. : 2411021-01-5

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生物活性

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

分子量

792.97

Formula

C43H56N10O5

CAS 号

2411021-01-5

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]. Wei D, et al. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J Med Chem. 2021 Oct 14;64(19):14822-14847.

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Bromo-C10-OBn

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。

Bromo-C10-OBn 

Bromo-C10-OBn 是一种可用于合成 PROTAC 的 PROTAC 连接子。

Bromo-C10-OBn

Bromo-C10-OBn Chemical Structure

CAS No. : 78277-30-2

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生物活性

Bromo-C10-OBn is a PROTAC linker that can be used in the synthesis of PROTACs.

分子量

355.31

Formula

C18H27BrO2

CAS 号

78277-30-2

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]. Powell CE, et al. Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC Med Chem. 2021 Jul 6;12(8):1381-1390.

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RAD51-IN-5

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。

RAD51-IN-5 

RAD51-IN-5 是一种有效的 RAD51 抑制剂。RAD51 是一种真核生物基因。RAD51-IN-5 具有研究线粒体缺陷病症的潜力 (摘自专利 WO2021164746A1,化合物 3)。

RAD51-IN-5

RAD51-IN-5 Chemical Structure

CAS No. : 2690367-19-0

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生物活性

RAD51-IN-5 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-5 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 3)[1].

分子量

550.73

Formula

C26H38N4O5S2

CAS 号

2690367-19-0

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]. Peng Gu, et al. Substituted aryl compound. Patent WO2021164746A1.

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S-(N-PhenethylthiocarbaMoyl)-L-cysteine(Synonyms: PEITC-Cys)

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。

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (Synonyms: PEITC-Cys)

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) 是一种抗癌物质 (anticarcinogenic),具有抗白血病活性。S-(N-PhenethylthiocarbaMoyl)-L-cysteine 抑制 HL60 细胞的 DNA 合成。S-(N-PhenethylthiocarbaMoyl)-L-cysteine 是 P450 抑制剂。

S-(N-PhenethylthiocarbaMoyl)-L-cysteine(Synonyms: PEITC-Cys)

S-(N-PhenethylthiocarbaMoyl)-L-cysteine Chemical Structure

CAS No. : 53330-02-2

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生物活性

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys), an anticarcinogenic agent, has antileukemic activity. S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells[1]. S-(N-PhenethylthiocarbaMoyl)-L-cysteine is a P450 inhibitor[2].

IC50 & Target

DNA Synthesis[1]; P450[2]

体外研究
(In Vitro)

S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits cell growth of HL60 cell (GC50=336 nM)[1].
S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells (IC50=6.47 μM)[1].
S-(N-PhenethylthiocarbaMoyl)-L-cysteine induced DNA fragmentation in HL 60 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.

Cell Proliferation Assay[1]

Cell Line: HL60 cells
Concentration: 0.1-10 μM
Incubation Time: 48 hours
Result: Inhibited the cell growth with a GC50 value of 336 nM.

Cell Proliferation Assay[1]

Cell Line: HL60 cells
Concentration: 4 μM
Incubation Time: 0, 20, 40, 60, 80, 100 hours
Result: Inhibited the cell growth.

分子量

284.40

Formula

C12H16N2O2S2

CAS 号

53330-02-2

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]. Adesida A, Edwards LG, Thornalley PJ. Inhibition of human leukaemia 60 cell growth by mercapturic acid metabolites of phenylethyl isothiocyanate. Food Chem Toxicol. 1996 Apr;34(4):385-92.

    [2]. Conaway CC, et al. Decomposition rates of isothiocyanate conjugates determine their activity as inhibitors of cytochrome p450 enzymes. Chem Res Toxicol. 2001 Sep;14(9):1170-6.

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PROTAC CDK9 ligand-1

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。

PROTAC CDK9 ligand-1 

PROTAC CDK9 ligand-1 是一种可用于合成 PROTAC 的 CDK9 配体。

PROTAC CDK9 ligand-1

PROTAC CDK9 ligand-1 Chemical Structure

CAS No. : 2411021-95-7

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生物活性

PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.

分子量

368.48

Formula

C20H28N6O

CAS 号

2411021-95-7

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]. Wei D, et al. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J Med Chem. 2021 Oct 14;64(19):14822-14847.

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Anticancer agent 64

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。

Anticancer agent 64 

Anticancer agent 64 (化合物 5m) 对 CCRF-CEM 细胞具有细胞毒性,其 IC50 为2.4 μM。Anticancer agent 64 通过诱导细胞凋亡表现出良好的抗癌活性。Anticancer agent 64 诱导 caspase 3 和 7 的激活和 PARP 的裂解。Anticancer agent 64 具有明显的线粒体去极化作用。

Anticancer agent 64

Anticancer agent 64 Chemical Structure

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生物活性

Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization[1].

IC50 & Target

Caspase 3

 

Caspase-7

 

Bcl-2

 

Bax

 

PARP

 

体外研究
(In Vitro)

Anticancer agent 64 (compound 5m) increases BAX expression and decreases Bcl-2 protein expression[1].
. Anticancer agent 64 shows significant increasement in cells accumulation in the G2/M phase of the cell cycle, while proportion of cells in S phase is reduced[1].

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

分子量

510.77

Formula

C31H46N2O2S

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]. Borková L, et al. Synthesis and biological evaluation of triterpenoid thiazoles derived from betulonic acid, dihydrobetulonic acid, and ursonic acid. Eur J Med Chem. 2020 Jan 1;185:111806.

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MNK/PIM-IN-1

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。

MNK/PIM-IN-1 

MNK/PIM-IN-1 是一种新型的 MNK/PIM 双抑制剂,具有良好的药代动力学特征。

MNK/PIM-IN-1

MNK/PIM-IN-1 Chemical Structure

CAS No. : 2430792-91-7

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生物活性

MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

分子量

486.54

Formula

C27H27FN6O2

CAS 号

2430792-91-7

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]. Han Y, et al. Optimization of 4,6-Disubstituted Pyrido[3,2-d]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth. J Med Chem. 2021 Sep 23;64(18):13719-13735.

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Branaplam hydrochloride(Synonyms: LMI070 hydrochloride; NVS-SM1 hydrochloride)

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。

Branaplam hydrochloride (Synonyms: LMI070 hydrochloride; NVS-SM1 hydrochloride)

Branaplam (LMI070; NVS-SM1) hydrochloride 是一种口服有效和选择性的 SMN2 拼接调节剂,对 SMN 的 EC50 为 20 nM。Branaplam hydrochloride 抑制 hERGIC50 为 6.3 μM。Branaplam hydrochloride 在严重的脊髓性肌萎缩症 (SMA) 小鼠模型中可提高全长 SMN 蛋白并延长其生存期。

Branaplam hydrochloride(Synonyms: LMI070 hydrochloride; NVS-SM1 hydrochloride)

Branaplam hydrochloride Chemical Structure

CAS No. : 1562338-39-9

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Branaplam hydrochloride 的其他形式现货产品:

Branaplam

生物活性

Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model[1][2].

体外研究
(In Vitro)

Branaplam (LMI070; NVS-SM1) hydrochloride treatment induces changes in the levels of 175 genes in human fibroblasts[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)

Branaplam (LMI070; NVS-SM1; 3, 10, 30 mg/kg; oral) hydrochloride produces dose-dependent elevations of SMN2-FL transcript and SMN protein in brain and spinal cord[1].
Branaplam (1 mg/kg of IV; 3 mg/kg of PO) hydrochloride has a CL of 25 mL/min/kg and an AUC of 3.03 μM•h[2].
A single Branaplam (oral; 30 mg/kg) hydrochloride results in significant and durable SMN protein elevation in brain for up to 160 hours in C/+ mice[1].
Branaplam (oral; 0.03, 0.1, 0.3, 1, 3 mg/kg) hydrochloride improves body weight and extendes lifespan in n SMNΔ7 mice[1].

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

分子量

429.94

Formula

C22H28ClN5O2

CAS 号

1562338-39-9

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.

溶解性数据
In Vitro: 

H2O : 200 mg/mL (465.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3259 mL 11.6295 mL 23.2591 mL
5 mM 0.4652 mL 2.3259 mL 4.6518 mL
10 mM 0.2326 mL 1.1630 mL 2.3259 mL

参考文献
  • [1]. Palacino J, et al. SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice. Nat Chem Biol. 2015 Jul;11(7):511-517.

    [2]. Cheung AK, et al. Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA). J Med Chem. 2018 Dec 27;61(24):11021-11036.

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Thio-ITP(Synonyms: 6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5′-triphosphate; 6-Thio-ITP)

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。

Thio-ITP (Synonyms: 6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5′-triphosphate; 6-Thio-ITP)

Thio-ITP (6-Thioinosine 5′-triphosphate) 是一种 RNA 聚合酶 (RNA polymerase) 活性的竞争性抑制剂。Thio-ITP 对聚合酶具有高表观亲和力,RNA 聚合酶 I 的 Ki 值为 40.9 μM,RNA聚合酶 II 的 Ki 值为 38.0 μM。

Thio-ITP(Synonyms: 6-Thioinosine 5′-triphosphate;  6-Mercaptopurine-riboside-5

Thio-ITP Chemical Structure

CAS No. : 27652-34-2

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生物活性

Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM)[1].

IC50 & Target[1]

RNA polymerase I

40.9±11.0 μM (Ki)

RNA polymerase II

38.0±6.47 μM (Ki)

体外研究
(In Vitro)

Thio-ITP inhibits both endogenous and exogenous DNA-directed RNA synthesis[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

524.23

Formula

C10H15N4O13P3S

CAS 号

27652-34-2

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]. Kawahata RT, Chuang LF, Holmberg CA, Osburn BI, Chuang RY. Inhibition of human lymphoma DNA-dependent RNA polymerase activity by 6-mercaptopurine ribonucleoside triphosphate. Cancer Res. 1983 Aug;43(8):3655-9.

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