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Tocris/Ro 31-8220 mesylate/2002/10/10 mg

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货号: 2002/10

品牌: Tocris

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Description: Protein kinase inhibitor

Alternative Names: Bisindolylmaleimide IX

Chemical Name: 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

Purity: ≥97% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Compound Libraries

Ro 31-8220 mesylate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	553.65
Formula	C₂₅H₂₃N₅O₂S.CH₃SO₃H
Storage	Desiccate at -20°C
Purity	≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	55.37	100
	ethanol	2.77	5

Preparing Stock Solutions

The following data is based on the product molecular weight 553.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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 insulin. Endocrinology 150 2145 PMID:

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