| Ro 31-8220 Mesylate Pan-PKC inhibitor |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | 138489-18-6 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | methanesulfonic acid;3-[3-[4-(1-methylindol-3-yl)-2,5-dioxopyrrol-3-yl]indol-1-yl]propyl carbamimidothioate | ||
| Canonical 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 | ||
| Formula | C25H23N5O2S.CH4O3S | M.Wt | 553.65 |
| Solubility | >27.7mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ro 31-8220 Mesylate is a selective inhibitor of protein kinase C (PKC) with IC50 values of 5, 24, 14, 27, and 24 nM for PKC α, PKC βI, PKC βII, PKC γ and PKC ε, respectively [1].
PKC is a monomeric Ca2+- and phospholipid-dependent Ser/Thr protein kinases and plays an important role in growth factor-activated signaling and malignant transformation.
Ro 31-8220 Mesylate is a selective inhibitor of PKC. Also, Ro 31-8220 increased growth factor-stimulated expression of c-Jun but inhibited MKP-1 and c-Fos expression. Ro-31-8220 strongly stimulated the stress-activated protein kinase JNK1 in a PKC-independent way [2]. In peripheral blood mononuclear cells, Ro 31-8220 inhibited the production of mitogen-induced interleukin (IL)-2 and IL-2-dependent T lymphoblast proliferation with IC50 values of 80 and 350 nM, respectively. Also, Ro 31-8220 (400 nM) inhibited IL-2Rα (CD25) expression by 27%, which suggested that Ro 31-8220 inhibited early and late T cell activation [3].
In rat adipocytes and L6 myotubes, RO 31-8220 activated c-Jun N-terminal kinase (JNK) and glycogen synthase (GS) and stimulated glucose incorporation into glycogen. While, RO 31-8220 inhibited the activity of extracellular response kinases 1 and 2 (ERK1/2) in a PKC-independent way [4].
References:
[1]. Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J, 1993, 294 ( Pt 2): 335-337.
[2]. Beltman J, McCormick F, Cook SJ. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem, 1996, 271(43): 27018-27024.
[3]. Geiselhart L, Conti DJ, Freed BM. RO 31-8220, a novel protein kinase C inhibitor, inhibits early and late T cell activation events. Transplantation, 1996, 61(11): 1637-1642.
[4]. Standaert ML, Bandyopadhyay G, Antwi EK, et al. RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin.