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抑制剂/激活剂

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凋亡与自噬

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BI-D1870

BI-D1870是一种ATP-竞争性S6 ribosome抑制剂，在无细胞试验中作用于RSK1/2/3/K4，IC50分别为31 nM/24 nM/18 nM/15 nM，作用于RSK比作用于MST2，GSK-3β，MARK3，CK1和Aurora B选择性高10到100倍。BI-D1870 显示除了抗癌的属性包括活性氧的生成、提高内质网应激反应和诱导自噬

货号：
TK0417
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	501437-28-1
生物活性	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.
分子式	C19H23F2N5O2
分子量	391.42
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 5 mg/mL (12.77 mM; Need ultrasonic)
体内研究	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.
体外研究	BI-D1870 inhibits a mutant of RSK2 lacking the C-terminal kinase catalytic domain (RSK2) with an IC50 of approx. 30 nM. BI-D1870 inhibits RSK1 and RSK2 with IC50 values of 10 nM and 20 nM respectively, when the kinase assays are performed with 100 μM ATP. When the assays are performed at a 10-fold lower ATP concentration, the IC50 of BI-D1870 is reduced to 5 nM for RSK1 and 10 nM for RSK2. BI-D1870 inhibits PLK1 with an IC50 of 100 nM, whilst the IC50 values for Aurora B, DYRK1a, CDK2-A, Lck, CK1 and GSK3β are 10- to 100-fold higher than that of the RSK isoforms. BI-D1870 (10 μM) inhibits the PMA-induced phosphorylation of GSK3α and GSK3β in HEK-293 cells. In HEK-293 cells, BI-D1870 inhibits the EGF-induced phosphorylation of LKB1 at Ser431 with an IC50 of approx. 1 μM. BI-D1870 does not affect the activation of ERK1/ERK2 and MSK1, nor does it inhibit the phosphorylation of CREB. BI-D1870 is a potent RSK family kinase inhibitor (Kds: 10-100 nM), and also interact with BRD4(1) and PLK family, with Kds of 3.5 μM and appr 10 nM. BI-D1870 (10 μM) strongly induces p70S6K activation in serum-starved LN-229 cells, and alao stimulates the phosphorylation of rpS6 and p70S6K in LN-18 cells. BI-D1870 (1 μM) potently inhibits rpS6 phosphorylation, and inhibits PMA-induced rpS6 phosphorylation at concentrations higher than 1 μM. BI-D1870 (1-5 μM) induces a dose- and time-dependent inhibition of cell proliferation in all cell types. BI-D1870 (1-3 μM) induces apoptosis in SCC4 cells and HSC-3 cells. BI-D1870 (0-5) modulates cell survival signaling pathways including Akt and p38 MAPK dose-dependently.
文献	•Theranostics. 2020 May 25;10(15):6915-6927. •Theranostics. 2019 Sep 21;9(24):7108-7121. •Oncogene. 2020 Oct;39(43):6733-6746. •Transl Res. 2021 Apr 19;S1931-5244(21)00084-0. •Viruses. 2018 Apr 13;10(4). pii: E191. •Programa de Doctorado en Biomedicina. 2020 Sep. •Oncotarget. 2016 Mar 1;7(9):10283-96. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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