目錄:MedChemExpress LLC>>信號通路>> AMG-548 dihydrochloride | MCE
| 純度 | 99.85% | 分子量 | 534.48 |
|---|---|---|---|
| 分子式 | C??H??Cl?N?O | 供貨周期 | 現貨 |
| 規(guī)格 | 1 mg | 貨號 | HY-108642B |
| 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產業(yè),制藥/生物制藥 |
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產品活性：AMG-548 dihydrochloride 是一種口服有效的，選擇性 p38α 抑制劑 (Ki=0.5 nM)，對 p38β 略有選擇性 (Ki=36 nM) 并且對 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 信號傳導。
研究領域：MAPK/ERK Pathway | Stem Cell/Wnt | Cell Cycle/DNA Damage
作用靶點：p38 MAPK | Casein Kinase
In Vitro: AMG-548 dihydrochloride shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 dihydrochloride has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=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 t1/2 is 4.6 hours in rats and 7.3 hours in dogs.
相關產品：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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