2. MAPK/ERK Pathway Stem Cell/Wnt Cell Cycle/DNA Damage
  3. p38 MAPK Casein Kinase
  4. AMG-548 hydrochloride

AMG-548 hydrochloride是一种口服有效的，选择性 p38α 抑制剂 (Ki=0.5 nM)，对 p38β 略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有 >1000 倍的选择性。AMG 548 hydrochloride也有效抑制全血 LPS 刺激的 TNFα (IC50=3 nM)。AMG-548 hydrochloride通过直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε 来抑制 Wnt 信号传导。

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AMG-548 hydrochloride Chemical Structure

AMG-548 hydrochloride Chemical Structure

CAS No. : 2437438-16-7

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AMG-548 hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of AMG-548 hydrochloride:

AMG-548 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 Casein Kinase 亚型特异性产品:

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CK1 CK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].

IC50 & Target[1][2]

p38α

0.5 nM (Ki)

p38β

3.6 nM (Ki)

p38δ

2600 nM (Ki)

p38γ

4100 nM (Ki)

dog p38α

5.0 nM (Ki)

JNK1

11480 nM (Ki)

JNK2

39 nM (Ki)

JNK3

61 nM (Ki)

CK1

 

体外研究
(In Vitro)

AMG-548 hydrochloride shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 hydrochloride has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC50=3 nM) and IL1b (IC50=7 nM) as well as TNFa induced IL-8 (IC50=0.7 nM) and IL-1b induced IL-6 (IC5050=1.3 nM) in human whole blood[1].
AMG-548 hydrochloride (10 μM) inhibits the hDvl2 shift[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AMG-548 hydrochloride 相关抗体:
体内研究
(In Vivo)

AMG-548 hydrochloride has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

498.02

Formula

C29H28ClN5O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AMG-548 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG-5482437438-16-7AMG548AMG 548p38 MAPKCasein Kinaseselectivep38αp38βTNFαWntdevelopmentstemcellsInhibitorinhibitorinhibit

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产品名称：
AMG-548 hydrochloride
目录号：
HY-108642A
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