1. MAPK/ERK Pathway
  2. MAP4K
  3. DMX-5804

DMX-5804 

目录号: HY-111754
产品使用指南

DMX-5804 是一种有效、可口服、选择性的 MAP4K4 抑制剂,对人 MAP4K4 的 IC50 值为 3 nM,pIC50 值为 8.55;对 MINK1/MAP4K6 (pIC50,8.18) 和 TNIK/MAP4K7 (pIC50,7.96) 的作用相对较弱。DMX-5804 能够增强心肌细胞存活率,减少小鼠的缺血再灌注损伤。

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DMX-5804 Chemical Structure

DMX-5804 Chemical Structure

CAS No. : 2306178-56-1

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     可免费申领三个不同产品的试用装。

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Description

DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice[1].

IC50 & Target[1]

MAP4K4

3 nM (IC50)

MAP4K4

8.55 (pIC50)

MINK1/MAP4K6

8.18 (pIC50)

TNIK/MAP4K7

7.96 (pIC50)

GCK/MAP4K2

6.50 (pIC50)

KHS/MAP4K5

6.36 (pIC50)

GLK/MAP4K3

4.95 (pIC50)

MLK1/MAP3K9

7.19 (pIC50)

MLK3/MAP3K11

6.99 (pIC50)

NUAK

6.88 (pIC50)

VEGFR

5.72 (pIC50)

ABL1

5.80 (pIC50)

Aurora B

5.49 (pIC50)

FLT3

5.31 (pIC50)

GSK3β

4.66 (pIC50)

In Vitro

DMX-5804 exhibits great selectivity at MAP4K4 over other kinases, such as GCK/MAP4K2 (pIC50, 6.50), GLK/MAP4K3 (pIC50, 4.95), KHS/MAP4K5 (pIC50, 6.36), ABL1 (pIC50, 5.80), Aurora B (pIC50, 5.49), FLT3 (pIC50, 5.31), GSK3β (pIC50, 4.66), MLK1/MAP3K9 (pIC50, 7.19), MLK3/MAP3K11 (pIC50, 6.99), NUAK (pIC50, 6.88) and VEGFR (pIC50, 5.72)[1].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (345.89 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7671 mL 13.8355 mL 27.6709 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 mL
10 mM 0.2767 mL 1.3835 mL 2.7671 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。
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References
Molecular Weight

361.39

Formula

C₂₁H₁₉N₃O₃

CAS No.

2306178-56-1

SMILES

O=C1NC=NC2=C1C(C3=CC=C(OCCOC)C=C3)=CN2C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere

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The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
DMX-5804
目录号:
HY-111754
需求量:

DMX-5804

Cat. No.: HY-111754