Ro 31-8220 mesylate

Cat. No. 2002 6 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Protein kinase inhibitor

别名： Bisindolylmaleimide IX

化学名： 3-[3-[2,5-Dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl carbamimidothioic acid ester mesylate

纯度： ≥97% (HPLC)

引用文献 (6)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Ro 31-8220 mesylate

Ro 31-8220 mesylate is a protein kinase C inhibitor, with activity at other protein kinases (IC₅₀ values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively). Activates JNK and glycogen synthase, and inhibits MAPK and ERK2, in rat adipocytes and L6 myotubes. Also inhibits voltage-dependent Na⁺ channels in the micromolar range. Induces protein-protein interaction between mutant SMAD4^R361H and SMAD3, leading to reactivation of dormant SMAD4^R361H-mediated transcriptional activity and restoration of TGF-β-induced tumor suppression activity in SMAD4 mutant cancer cells.

化合物库 for Ro 31-8220 mesylate

Ro 31-8220 mesylate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for Ro 31-8220 mesylate

分子量	553.65
公式	C₂₅H₂₃N₅O₂S.CH₃SO₃H
储存	Desiccate at -20°C
纯度	≥97% (HPLC)
CAS Number	138489-18-6
PubChem ID	11628205
InChI Key	SAWVGDJBSPLRRB-UHFFFAOYSA-N
Smiles	CS(O)(=O)=O.CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CN(CCCSC(N)=N)C2=CC=CC=C12

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Ro 31-8220 mesylate

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	55.37	100
	ethanol	2.77	5

制备储备液 for Ro 31-8220 mesylate

以下数据基于产品分子量 553.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.81 mL	9.03 mL	18.06 mL
5 mM	0.36 mL	1.81 mL	3.61 mL
10 mM	0.18 mL	0.9 mL	1.81 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

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产品说明书 for Ro 31-8220 mesylate

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Ro 31-8220 mesylate

参考文献是支持产品生物活性的出版物。

Davis et al (1989) Potent, selective inhibitors of protein kinase C. FEBS Lett. 259 61 PMID: 2532156

Lingameneni et al (2000) Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS Lett. 473 265 PMID: 10812087

Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351

Standaert et al (1999) RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of Ins. Endocrinology 150 2145 PMID: 10218965

Tang et al (2020) Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-β signaling. Cell Chem.Biol. S2451-9456 30473 PMID: 33326750

If you know of a relevant reference for Ro 31-8220 mesylate, please let us know.

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