BI-D1870 - CAS:501437-28-1

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BI-D1870

目录号 : KM2626 CAS No. : 501437-28-1 纯度 : 98%

Data Sheet 产品使用指南

BI-D1870 是ATP 竞争性的，细胞可渗透性的、能透过血脑屏障的 RSK 抑制剂，抑制 RSK1、RSK2、RSK3、RSK4 的 IC₅₀ 值分别为 31 nM、24 nM、18 nM、15 nM。

规格	价格	是否有货	数量
2mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

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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.

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 (K_ds: 10-100 nM), and also interact with BRD4(1) and PLK family, with K_ds 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.

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.

分子式

C₁₉H₂₃F₂N₅O₂

分子量

391.42

CAS号

501437-28-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 5 mg/mL (12.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5548 mL	12.7740 mL	25.5480 mL
5 mM	0.5110 mL	2.5548 mL	5.1096 mL
10 mM	0.2555 mL	1.2774 mL	2.5548 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.39 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.39 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.39 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 8 篇科研文献

The molarity calculator equation

The dilution calculator equation