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DTP3 {[allProObj[0].p_purity_real_show]}

货号:A813133 Ambeed 开学季,买赠积分,赢豪礼

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway.

DTP3 化学结构 CAS号:1809784-29-9
DTP3 化学结构
CAS号:1809784-29-9
DTP3 3D分子结构
CAS号:1809784-29-9
DTP3 化学结构 CAS号:1809784-29-9
DTP3 3D分子结构 CAS号:1809784-29-9
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DTP3 纯度/质量文件 产品仅供科研

货号:A813133 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

{[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。

DTP3 生物活性

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].

DTP3 动物研究

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].

DTP3 参考文献

[1]Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.

[2]Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508.

DTP3 实验方案

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

DTP3 技术信息

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
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