Ro 31-8220

Name: Ro 31-8220
Brand: TargetMol
SKU: T6643L
Rating: 4.5 (1 reviews)

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产品编号 T6643LCas号 125314-64-9

Ro 31-8220 是一种有效的PKC 抑制剂，对 PKCα，PKCβI，PKCβII，PKCγ，PKCε 和大鼠大脑 PKC 的IC50值为 5，24，14，27，24 和 23 nM。Ro 31-8220还显著抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β，IC50值分别为3，8，15，38 nM，对 MKK3，MKK4，MKK6 和 MKK7 无作用。

Ro 31-8220

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产品编号 T6643LCas号 125314-64-9

规格	价格	库存
25 mg	¥ 10,600	1-2周
50 mg	¥ 13,800	1-2周
100 mg	¥ 17,500	1-2周

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产品描述	Ro 31-8220 is a potent inhibitor of PKC with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β with IC50s of 3, 8, 15, and 38 nM, respectively without effect on MKK3, MKK4, MKK6 and MKK7.
靶点活性	GSK-3β:38 nM, PKCβII:14 nM, PKCγ:27 nM, PKC (rat brain):23 nM, PKCε:24 nM, MSK1:8 nM, MAPKAP-K1b:3 nM, PKCβI:24 nM, PKCα:5 nM, S6K1:15 nM
体外活性	Ro 31-8220 is a potent PKC inhibitor, with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively [1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC 50 s, 3, 8, 15, and 38 nM, respectively), without effect on MKK3, MKK4, MKK6 and MKK7. Furthermore, Ro 31-8220 directly suppresses voltage-dependent Na + channels [2]. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels [3].
体内活性	Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP / mice show a significant rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change [4].