RepSox (Synonyms:E-616452; SJN 2511)
目录号 : KM7551 CAS No. : 446859-33-2 纯度 : 98%

RepSox (E-616452) 是一种有效,选择性的 TGFβR-1/ALK5 抑制剂, 抑制ALK5自磷酸化,IC50 为 4 nM。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with an IC50 of 4 nM.

体外研究

RepSox also inhibits ATP binding to ALK5 with IC50 of 23 nM. RepSox shows potent activity in both binding and cellular assays and exhibits selectivity over p38 mitogen-activated protein kinase. with IC50 of >16 μM. RepSox act s as an inhibitor of the Tgfβ1 kinase. Treatment with 25 μM RepSox almost completely eliminates Smad3 phosphorylation, indicating that RepSox strongly inhibits Tgfβ signaling in somatic cells. RepSox is most effective at replacing Sox2 during days 10-11 after transduction and that therefore cultures of Oct4, Klf4, and cMyc-transduced MEFs give rise to intermediates capable of responding to RepSox treatment. These intermediates appear at day 4 post-transduction and peak at days 10-11. Treatment with RepSox decreased the proportion of cells in G2/M phase of the cell cycle, indicating it does not increase the proliferation rate of these partially reprogrammed cells.

分子式
C17H13N5
分子量
287.32
CAS号
446859-33-2
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 : 33.33 mg/mL (116.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4804 mL 17.4022 mL 34.8044 mL
5 mM 0.6961 mL 3.4804 mL 6.9609 mL
10 mM 0.3480 mL 1.7402 mL 3.4804 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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (26.10 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (26.10 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution

  • 4.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution

  • 5.

    请依序添加每种溶剂: 1% DMSO    99% saline

    Solubility: ≥ 0.33 mg/mL (1.15 mM); Clear solution

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