| 產(chǎn)品描述： | BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively |
| 靶點(diǎn)： |
IC50: 31 nM (RSK1), 24 nM (RSK2), 18 nM (RSK3), 15 nM (RSK4);S6Kinase;Autophagy |
| 體內(nèi)研究： |
BI-D1870 (0.5 mg/kg)-injected experimental autoimmune encephalomyelitis (EAE) mice exhibits a delayed neural deficit without obvious weight loss. Histopathological analyses shows inflammatory cell infiltration and demyelination in the spinal cord in control mice, but not in BI-D1870-treated mice. BI-D1870 protects against the infiltration of TH1 or TH17 cells into the CNS |
| 參考文獻(xiàn)： |
1. Sapkota GP, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38. 2. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. 3. Takada I, et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221(2):188-92. 4. Roffe M, et al. Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. Cell Signal. 2015 Aug;27(8):1630-42. 5. Chiu CF, et al. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. |
| 溶解性： |
DMSO : 5 mg/mL (12.77 mM; Need ultrasonic) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.555 ml |
12.774 ml |
25.548 ml |
| 5 mM |
0.511 ml |
2.555 ml |
5.11 ml |
| 10 mM |
0.255 ml |
1.277 ml |
2.555 ml |
| 50 mM |
0.051 ml |
0.255 ml |
0.511 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京