DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway.
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产品名称 | MEK ↓ ↑ | MEK1 ↓ ↑ | MEK1/2 ↓ ↑ | MEK2 ↓ ↑ | MEK5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mirdametinib |
++++
MEK, IC50: 0.33 nM |
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Binimetinib |
+++
MEK, IC50: 12 nM |
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BI-847325 |
++
MEK1, IC50: 25 nM |
+++
MEK2, IC50: 4 nM |
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U0126-EtOH |
+
MEK1, IC50: 0.07 μM |
++
MEK2, IC50: 0.06 μM |
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GDC-0623 |
++++
MEK1, IC50: 0.13 nM |
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TAK-733 |
++++
MEK1, IC50: 3.2 nM |
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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 |
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CI-1040 |
++
MEK1, IC50: 17 nM |
++
MEK2, IC50: 17 nM |
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Myricetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Refametinib |
++
MEK1, IC50: 19 nM |
++
MEK2, IC50: 47 nM |
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Cobimetinib |
+++
MEK1, IC50: 4.2 nM |
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PD98059 |
+
MEK1, IC50: 2 μM |
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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 |
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(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。 |
描述 | DTP3 acts as a powerful, selective inhibitor of GADD45β/MKK7. It is designed to engage a critical, cancer-specific survival mechanism that operates downstream from the NF-κB signaling pathway[1]. Administering DTP3 at a concentration of 10 μM for a duration ranging from 1 to 21 days leads to a robust and selective triggering of JNK activation and cell death via apoptosis. This is evidenced by the detection of phosphorylated JNK within 24 hours of treatment[2]. |
Animal study | DTP3, when administered subcutaneously at a dose of 14.5 mg/kg/day for 28 days, has been observed to significantly reduce tumor size and effectively eliminate established subcutaneous myeloma xenografts in mice. Additionally, DTP3 administered via intravenous injection at 10 mg/kg/day exhibits a half-life (t1/2) of 1.26 hours, a clearance rate (CL) of 27.13 mL/min/kg, and a volume of distribution (Vd) of 2.80 L/kg[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.90mL 0.38mL 0.19mL |
9.51mL 1.90mL 0.95mL |
19.03mL 3.81mL 1.90mL |
CAS号 | 1809784-29-9 |
分子式 | C26H35N7O5 |
分子量 | 525.6 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(199.77 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 H2O: 100 mg/mL(190.26 mM) |
动物实验配方 |