BI-D1870

SKU: orb1301013

特色

描述

BI-D1870

研究领域

Cell Biology, Immunology & Inflammation, Neuroscience, Stem Cell & Developmental Biology

图片与验证

−

关键属性

−

CAS 号	501437-28-1
MW	391.42
纯度	>98%
分子式	C₁₉H₂₃F₂N₅O₂
SMILES	CC(C)CCN1C(C)C(=O)N(C)c2cnc(Nc3cc(F)c(O)c(F)c3)nc12
靶点	Kinase
溶解性	Soluble in DMSO (up to 15 mg/ml)

生物活性

−

靶点 IC50	RSK3:18 nM (cell free)\|RSK2:24 nM (cell free)\|RSK1:31 nM (cell free)\|RSK4:15 nM (cell free)
体内	METHODS: Two days after immunization with MOG peptide, BI-D1870 (0.5 mg/kg) was injected intraperitoneally into mice and repeated every other day for 11 days. RESULTS Mice showed delayed neurological deficits; BI-D1870 treatment had a moderate protective effect against weight loss.
体外	METHODS: HEK-293 cells were incubated with BI-D1870 (10 μM, 15 min, 4 h total) To examine whether BI-D1870 could inhibit RSK activity in cells, the effect of BI-D1870 on RSK-catalyzed phosphorylation of its known substrates in HEK-293 cells was investigated using PMA as an agonist to activate ERK1/ERK2 and RSK isoforms. RESULTS Incubation of cells with BI-D1870 significantly inhibited PMA-induced phosphorylation of GSK3α and GSK3β. In contrast, BI-D1870 had little effect on PMA-induced activation of ERK1/ERK2 (catalyzed by Raf and MKK1) or phosphorylation of CREB at Ser at any time point. METHODS: Oral cancer cell lines (SCC2095, SCC4, SCC9, Ca922 and HSC-3) and NHOK cells were treated with BI-D1870 (1, 2, 3, 4, 5.28 or 48 hours), and the growth of these cells was detected by MTT. RESULTS BI-D1870 showed a dose-responsive antiproliferative effect on OSCC cells. METHODS: Cells transfected with immunofluorescent GFP-LC3 were treated with BI-D1870 (0.5, 2 μM) for 48 hours and observed under a confocal microscope; DAPI staining was used to locate the nucleus, and Western blot of LC3B was observed in cells treated with BI-D1870 for 48 hours. RESULTS BI-D1870 induced autophagy, and Western blot of LC3B-II showed that this induction was dose-dependent.
细胞研究	The rat embryo fibroblast cell line, Rat-2 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% (v/v) FBS. HEK-293 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% FBS and 1×antimycotic/antibiotic solution. Prior to stimulation, cells were cultured in the absence of serum for 16 h. Inhibitors were dissolved in DMSO at a 1000-fold higher concentration than they were used at. These inhibitors, or the equivalent volume of DMSO as a control, were added to the tissue culture medium 30 min prior to stimulation unless indicated otherwise. The final concentration of DMSO in the culture medium was 0.1% and had no effect on agonist-induced activation or phosphorylation of any of the substrates examined. The cells were stimulated with the indicated agonists and lysed in 1 ml of ice-cold Lysis Buffer and centrifuged at 16000 g at 4 °C for 5 min. The supernatants were frozen in liquid nitrogen and stored at 80 °C until use. Protein concentrations were determined using the Bradford method with BSA as the standard .
动物研究	Myelin oligodendrocyte glycoprotein (MOG) peptide 35–55. (MEVGWYRSPFSRVVHLYRNGK) (BEX) was used to induce EAE in C57/BL6J mice. Mice were injecteds.c. with 200 g of MOG peptide in100 L of PBS emulsified in 100 L complete Freund's adjuvant (CFA) that was further supplemented with five mg mL 1 Mycobacterium tuberculosis (H37Ra). In addition, 500 ng pertussis toxin was injected i.p. on days zero and two. The RSK inhibitor (BI-D1870; 0.5 mg kg 1) was injected i.p. into mice two days after immunization with MOG peptide, and injection was repeated every other day for 11 days. Mice that received only dimethyl sulfoxide (DMSO) solution were used as controls. Paralysis was evaluated according to the following scale: zero, no disease; one, tail limpness; two, hind limb weakness; three, hind limb paralysis; four, forelimb weakness; five, quadriplegia; six, death. For histological analysis, CNS samples were fixed with 4% paraformaldehyde and sliced at 4 m, and then hematoxylin & eosin (H & E) staining was performed .

储存与操作

−

储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

−

S6Kinase, S6 Kinase, S6K, RSK2, RSK4, RSK1, RSK3, Ribosomal S6 Kinase (RSK), inhibit, Inhibitor, Autophagy, BI D1870, BI-D 1870, BID1870, BI-D1870, BI-D-1870

相似产品

−

Binimetinib [orb1224490]
纯度：
>98% (HPLC)
CAS 号：
606143-89-9
MW:
441.23
分子式：
C₁₇H₁₅BrF₂N₄O₃
可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g
BI-D1870 [orb1224926]
纯度：
>98% (HPLC)
CAS 号：
501437-28-1
MW:
391.42
分子式：
C₁₉H₂₃F₂N₅O₂
可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

25023738 ↗

关键属性

−

暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98% (HPLC)
CAS 号：	606143-89-9
MW:	441.23
分子式：	C₁₇H₁₅BrF₂N₄O₃

BI-D1870

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Binimetinib [orb1224490]

BI-D1870 [orb1224926]

质量保证

化合物标识

关键属性

实验方案信息

可选规格