Ro 31-8220 CAS: 138489-18-6
MF: C25H23N5O2S•CH4O3S
MW: 553.65
A cell-permeable PKC inhibitor that has been shown to be selective for PKC over CaM kinase II and PKA.

Ro 31-8220 (CAS 138489-18-6)

Ro 31-8220 | CAS 138489-18-6 is rated 5.0 out of 5 by 1.
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Alternate Names: Bisindolylmaleimide IX, Methanesulfonate
Application: Ro 31-8220 is a cell-permeable PKC inhibitor that has been shown to be selective for PKC over CaM kinase II and PKA
CAS Number: 138489-18-6
Purity: ≥98%
Molecular Weight: 553.65
Molecular Formula: C25H23N5O2S•CH4O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ro 31-8220, a staurosporine (sc-3510) analog, is a cell-permeable inhibitor of PKC (protein kinase C) isoforms PKC α, PKC βI, PKC βII, PKC γ, and PKC ε (IC50 = 5, 24, 14, 27, and 24 nM, respectively). Ro 31-8220 has also been shown to induce apoptosis in various cell lines, independent of its PKC activity, and to inhibit GSK 3 (IC50 = 6.8nM). Ro 31-8220 is an inhibitor of Cdk2, cyclin A, GSK-3β, MSK1, Pim-3, Polycystin-1, PRK2, Rsk-1 and Rsk-2 and an activator of JNK1.


References

1. McKenna, J.P., et al. 1993. Biochem. Pharmacol. 46: 583-588. PMID: 8363630
2. Shen, L. and Glazer, R.I. 1998. Biochem. Pharmacol. 55: 1711-1719. PMID: 9634008
3. Hers, I., et al. 1999. FEBS Lett. 460: 433-436. PMID: 10556511
4. Han, Z., et al. 2000. Cell Death Differ. 7: 521-530. PMID: 10822275
5. Galkina, S.I., et al. 2010. Cell Adh Migr. 4: 32-38. PMID: 20009568

Physical State :
Solid
Solubility :
Soluble in water (7.3 mg/ml), DMSO (10 mg/ml), and ethanol (5 mM).
Storage :
Store at -20° C
Melting Point :
164-165.2° C
IC50 :
protein kinase C: IC50 = 10 nM; CaM kinase II: IC50 = 17 µM; protein kinase A: IC50 = 900 µM; GSK-3 in primary adipocytes: IC50 = 6.8 nM; GSK-3 in GSK-3β immunoprecipitates: IC50 = 2.8 nM
pK Values :
pKa: 7.90, pKb: 8.67
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
MDL Number :
MFCD03788207
SMILES :
CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N.CS(=O)(=O)O

Download SDS (MSDS)

Certificate of Analysis

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Ro 31-8220 (CAS 138489-18-6)  Product Citations

See how others have used Ro 31-8220 (CAS 138489-18-6). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 15 total

PMID: # 33785524  Khera, L.|Vinik, Y.|Maina, F.|Lev, S.| et al. 2021. Life Sci Alliance. 4:

PMID: # 27165344  Thomas, L. et al. 2016. Kidney & blood pressure research. 41: 298-310.

PMID: # 27793751  Tenconi, PE. et al. 2016. Int. J. Biochem. Cell Biol. 81: 67-75.

PMID: # 27543462  Sulen, A. et al. 2016. Pharmacol. Res. 113: 216-227.

PMID: # 26689644  Ojani, R. et al. 2016. Insect Biochem. Mol. Biol. 70: 44-52.

PMID: # 27746193  Gao, J.|Bai, T.|Ren, L.|Ding, Y.|Zhong, X.|Wang, H.|Guo, Y.|Li, J.|Liu, Y.|Zhang, Y.| et al. 2016. Peptides. 86: 72-79.

PMID: # 25980739  Sahu, G. et al. 2015. Virology. 483: 185-202.

PMID: # 26013540  Tang, R.|Gao, L.|Kawatani, M.|Chen, J.|Cao, X.|Osada, H.|Xiang, L.|Qi, J.| et al. 2015. Mol Pharmacol. 88: 326-34.

PMID: # 26416856  Euba, B. et al. 2015. Antimicrob. Agents Chemother. 59: 7581-92.

PMID: # 25014309  Pandeló José, D. et al. 2014. Virology. 462-463: 328-39.

Citations 1 to 10 of 15 total

does it cross the blood brain barrier

Asked by: Shyam
Thank you for your question. We have not been able to confirm whether or not o 31-8220 (CAS 138489-18-6) can cross the blood brain barrier. However, we would like to share some references with you that may be helpful in your research on this chemical. Potent selective inhibitors of protein kinase C: P.D. Davis, et al.; FEBS Lett. 259, 61 (1989) RO 31-8220 and RO 31-7549 show improved selectivity for protein kinase C over staurosporine in macrophages: P. Dieter & E. Fitzke; BBRC 181, 396 (1991) Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C: S.E. Wilkinson, et al.; Biochem. J. 294, 335 (1993)
Answered by: Technical Support
Date published: 2017-02-03

What is the solubility of this product?

Asked by: hawkeye11
Thank you for your question. The compound, sc-200619, is soluble in water (7.3 mg/mL), DMSO (10 mg/mL), and ethanol (5 mM). If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing [email protected], or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-07-11
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Rated 5 out of 5 by from Galkina et al Galkina et al. (PubMed ID 20009568) found that the microbial alkaloid Ro 31-8220, led to the development of membrane tubular extensions in human neutrophils following adhesion to fibronectiv-coated substrata. -SCBT Publication Review
Date published: 2015-03-11
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