货号:A934694 同义名: ASK1 Inhibitor 10
ASK1 Inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1). It is selective for ASK1 over ASK2 as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF. It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner.
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产品名称 | MEK ↓ ↑ | MEK1 ↓ ↑ | MEK1/2 ↓ ↑ | MEK2 ↓ ↑ | MEK5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
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Honokiol | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mirdametinib |
++++
MEK, IC50: 0.33 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Binimetinib |
+++
MEK, IC50: 12 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BI-847325 |
++
MEK1, IC50: 25 nM |
+++
MEK2, IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
U0126-EtOH |
+
MEK1, IC50: 0.07 μM |
++
MEK2, IC50: 0.06 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
GDC-0623 |
++++
MEK1, IC50: 0.13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
TAK-733 |
++++
MEK1, IC50: 3.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Trametinib |
++++
MEK1, IC50: 0.92 nM |
++++
MEK2, IC50: 1.8 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Selumetinib |
+++
MEK1, Kd: 99 nM MEK1, IC50: 14 nM |
+
MEK2, Kd: 530 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
CI-1040 |
++
MEK1, IC50: 17 nM |
++
MEK2, IC50: 17 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Myricetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Refametinib |
++
MEK1, IC50: 19 nM |
++
MEK2, IC50: 47 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Cobimetinib |
+++
MEK1, IC50: 4.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PD98059 |
+
MEK1, IC50: 2 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SL327 |
+
MEK1, IC50: 0.18 μM |
+
MEK2, IC50: 0.22 μM |
AP-1 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
PD318088 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
AZD8330 |
+++
MEK1/2, IC50: 7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pimasertib | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
(E/Z)-BIX02189 |
++++
MEK5, IC50: 1.5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(E/Z)-BIX02188 |
+++
MEK5, IC50: 4.3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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。 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03696446 | Coronary Heart Disease | Not Applicable | Recruiting | December 31, 2020 | Canada, Ontario ... 展开 >> University of Ottawa Heart Institute Recruiting Ottawa, Ontario, Canada, K1Y 4W7 Contact: Evyanne Wooding 613-696-7000 ext 17596 ewooding@ottawaheart.ca 收起 << |
NCT02267096 | Smoking Lung ... 展开 >>Cancer 收起 << | Phase 3 | Completed | - | United States, District of Col... 展开 >>umbia Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Massachusetts Lahey Hospital and Medical Center Burlington, Massachusetts, United States, 01805 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 收起 << |
NCT03107247 | Skeletal Injury | Phase 4 | Enrolling by invitation | March 31, 2021 | United States, Massachusetts ... 展开 >> Boston Children's Hospital Boston, Massachusetts, United States, 02115 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.31mL 0.46mL 0.23mL |
11.56mL 2.31mL 1.16mL |
23.13mL 4.63mL 2.31mL |
CAS号 | 1005775-56-3 |
分子式 | C21H23Cl2N5O |
分子量 | 432.346 |
别名 | ASK1 Inhibitor 10 |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(242.86 mM),配合低频超声助溶,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 |
动物实验配方 |