1. Epigenetics
    TGF-beta/Smad
  2. PKC

Ro 31-8220 mesylate (Synonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate)

Cat. No.: HY-13866 Purity: 99.50%
Data Sheet SDS Handling Instructions

Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

For research use only. We do not sell to patients.
Ro 31-8220 mesylate Chemical Structure

Ro 31-8220 mesylate Chemical Structure

CAS No. : 138489-18-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
10 mg USD 180 In-stock
50 mg USD 540 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of Ro 31-8220 mesylate:

  • Biological Activity

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  • Technical Information

  • Purity & Documentation

  • References

Description

Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively. IC50 Value: 5, 24, 14, 27, and 24 nM (PKC α, PKC βI, PKC βII, PKC γ, and PKC) [1] Target: pan-PKC 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. Ro 31-8220 antagonized (IC50, 1.0 microM) the effect of the activator of protein kinase C,12-O-tetradecanoylphorbol 13-acetate (TPA), on histamine-stimulated aminopyrine accumulation. Ro 31-8220 (0.1-2.14 microM) inhibited the aminopyrine response to 0.1 mM carbachol (IC50, 0.78 microM; 49% inhibition at 2.14 microM Ro 31-8220) and shifted the dose-response curve for the effect of carbachol concentration of aminopyrine accumulation downwards and to the right. No inhibition of aminopyrine accumulation induced by histamine was found with Ro 31-8220 (0.1-2.14 microM) [1]. U-87 and A172 cells treated with an IC50 of Ro 31-8220 exhibited nucleosomal DNA fragmentation that coincided with an increase in the number of apoptotic cells. This effect was preceded by the rapid nuclear accumulation of wild-type p53 within 2 hr, and an increased level of the pro-apoptotic protein, insulin-like growth factor-1-binding protein-3, (IGFBP3) but not other p53-regulated proteins such as p21WAF1 or Bax [2].

References
Molecular Weight

553.65

Formula

C₂₆H₂₇N₅O₅S₂

CAS No.

138489-18-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Ro 31-8220 mesylate
Cat. No.:
HY-13866
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