TA-02

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TA-02  纯度: 99.57%

TA-02 是 SB 203580 (HY-10256) 的一个类似物,是 p38 MAPK 的抑制剂,其 IC50 值为 20 nM。TA-02 可抑制 TGFBR-2。TA-02 和 SB 203580、SB 202190 (HY-10295) 具有相似的心源活性。

TA-02

TA-02 Chemical Structure

CAS No. : 1784751-19-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880 In-stock
1 mg ¥500 In-stock
5 mg ¥1200 In-stock
10 mg ¥2000 In-stock
50 mg ¥6000 In-stock
100 mg ¥8000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

TA-02, an analog of SB 203580 (HY-10256), is a p38 MAPK inhibitor with an IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. TA-02 exhibits similar cardiogenic properties as SB 203580 and SB 202190 (HY-10295)[1].

体外研究
(In Vitro)

TA-02 (5 μM) inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis. TA-02 at 5 μM concentration induces cardiogenesis, but also increases ATF-2 phosphorylation and MEF2C õexpression in contrast to what would be expected with a mechanism dependent on p38α MAPK inhibition[1].
TA-02 induces T/Brachyury whereas SB203580 addition increased MESP1 and T/Brachyury transcripts[1].
TA-02 significantly induces high NKX2-5 expression when applied between days 0-8[1].
TA-02 is found to inhibit multiple targets with similar potency to p38α MAPK, such as p38α, p38β, JNK3, JNK2, CIT, CK1ε, DMPK2, JNK1, DDR1 CK1δ, MEK5, and ERBB2[1].
TA-02 and SB203580 reduce the nuclear TCF/LEF-1 driven transcription of luciferase similar to DKK-1[1].
TA-02 (5 nM-5 μM) inhibits p38 and increases the anti-inflammation effects of BDNF on inflammation in vitro[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: The nerve cell line AGE1.HN.
Concentration: 5 nM-5 μM.
Incubation Time: 44 h (100 ng/ml LPS for 4 h at 37°C).
Result: Suppressed p-38 protein expression, reduced IL-1β, IL-6, IL-18 and TNF-α levels and inhibited iNOS and COX-2 levels in an in vitro model of SCI by BDNF overexpression, compared with the BDNF overexpression group.

分子量

333.33

Formula

C20H13F2N3

CAS 号

1784751-19-4

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 : 25 mg/mL (75.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0000 mL 15.0002 mL 30.0003 mL
5 mM 0.6000 mL 3.0000 mL 6.0001 mL
10 mM 0.3000 mL 1.5000 mL 3.0000 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 (7.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.50 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.50 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Laco F, et al. Cardiomyocyte differentiation of pluripotent stem cells with SB203580 analogues correlates with Wnt pathway CK1 inhibition independent of p38 MAPK signaling. J Mol Cell Cardiol. 2015 Mar;80:56-70.

    [2]. Jiedong Liang, et al. The activation of BDNF reduced inflammation in a spinal cord injury model by TrkB/p38 MAPK signaling. Exp Ther Med. 2019 Mar;17(3):1688-1696.

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