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产品名称 | STAT1 ↓ ↑ | STAT3 ↓ ↑ | STAT5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Nifuroxazide | ✔ | 98% | |||||||||||||||||
Fludarabine | ✔ | 98% | |||||||||||||||||
Artesunate | ✔ | 98% | |||||||||||||||||
BP-1-102 |
+++
STAT3, Kd: 504 nM |
99%+ | |||||||||||||||||
Niclosamide |
++
STAT3, IC50: 0.7 μM |
98% | |||||||||||||||||
Napabucasin | ✔ | 98% | |||||||||||||||||
Cryptotanshinone |
++
STAT3, IC50: 4.6 μM |
98% | |||||||||||||||||
Stattic |
+
STAT3, IC50: 5.1 μM |
98% | |||||||||||||||||
NSC 74859 |
+
STAT3, IC50: 86 μM |
99%+ | |||||||||||||||||
Ochromycinone | ✔ | 98% | |||||||||||||||||
HO-3867 | ✔ | 97% | |||||||||||||||||
C188-9 |
++++
STAT3, Kd: 4.7 nM |
99%+ | |||||||||||||||||
HJC0152 | ✔ | 99% | |||||||||||||||||
SH5-07 | ✔ | 97% | |||||||||||||||||
SH-4-54 |
++++
STAT3, Kd: 300 nM |
+++
STAT5, Kd: 464 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | STAT6 (signal transducers and activators of transcription 6) protein is activated by IL-4 and IL-13, and plays an important role in Th2 cells (T-helper cell 2) differentiation, which might make it an excellent therapeutic target for various allergic conditions, including asthma and atopic diseases. AS1517499 is a STAT6 inhibitor with IC50 value of 21nM, and also inhibited IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM, but has no effect on the ability of spleen T cells to produce IFN-γ, which is a marker of Th1 differentiation. AS1517499 could inhibit IL-13–induced activation of STAT6 and up-regulation of RhoA in cultured hBSMCs at concentration of 100nM. Intraperitoneal injections of AS1517499 at dose of 10mg/kg 1h before each exposure to ovalbumin could almost completely inhibit both the antigen-induced up-regulation of RhoA and bronchial smooth muscle hyperresponsiveness in mice. |
Dose | Mice: 1 mg/kg, 10 mg/kg[1] (i.p.), 20 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.51mL 0.50mL 0.25mL |
12.57mL 2.51mL 1.26mL |
25.13mL 5.03mL 2.51mL |
CAS号 | 919486-40-1 |
分子式 | C20H20ClN5O2 |
分子量 | 397.86 |
SMILES Code | O=C(C1=CN=C(NCCC2=CC=C(O)C(Cl)=C2)N=C1NCC3=CC=CC=C3)N |
MDL No. | MFCD24038757 |
别名 | |
运输 | 蓝冰 |
InChI Key | OZRMEKAUZBKTTC-UHFFFAOYSA-N |
Pubchem ID | 10340781 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
溶解方案 |
DMSO: 35 mg/mL(87.97 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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