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AMG-548 dihydrochloride

產(chǎn)品活性：AMG-548 dihydrochloride 是一種口服有效的，選擇性 p38α 抑制劑 (K_i=0.5 nM)，對(duì) p38β 略有選擇性 (K_i=36 nM) 并且對(duì) p38γ 和 p38δ 具有 >1000 倍的選擇性。AMG-548 dihydrochloride 也有效抑制全血 LPS 刺激的 TNFα (IC₅₀=3 nM)。AMG-548 dihydrochloride 通過直接抑制酪蛋白激酶 1 (Casein kinase 1) 同種型 δ 和 ε 來抑制 Wnt 信號(hào)傳導(dǎo)。

研究領(lǐng)域：MAPK/ERK Pathway  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage

作用靶點(diǎn)：p38 MAPK  |  Casein Kinase

In Vitro: AMG-548 dihydrochloride shows >1000 fold selective against p38γ (K_i=2600 nM) and p38δ (k_i=4100 nM). AMG-548 dihydrochloride has an modest selectivity against JNK2 (k_i=39 nM) and JNK3 (k_i=61 nM). AMG-548 dihydrochloride 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.
AMG-548 dihydrochloride (10 μM) inhibits the hDvl2 shift.

In Vivo: AMG-548 dihydrochloride has rat F of 62% and dog F of 47%. The t_1/2 is 4.6 hours in rats and 7.3 hours in dogs.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Pyroptosis Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Antidepressant Compound Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  CK2-IN-4  |  Umbralisib hydrochloride  |  Bisabolangelone  |  4-Hydroxylonchocarpin  |  TLR4/NF-κB/MAPK-IN-1  |  Broussonin E  |  L-threo-Sphingosine  |  4,5,6,7-Tetrabromo-1H-benzimidazole  |  SB 242235  |  Hydrangenol  |  JNJ-6204  |  CK2-IN-1  |  EGF-R (661-681) T669 Peptide  |  PF-5006739  |  TA-01  |  Ellagic acid  |  EGFR-IN-57  |  AMG-548 hydrochloride  |  JX401  |  Ganoderterpene A  |  VX-702  |  CKI-7 free base  |  Esculin  |  SR-1277  |  R1487 Hydrochloride  |  Emprumapimod  |  BMS-751324  |  CK2α-IN-1  |  NCC007  |  Emodin-d₄

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