| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D408878-1ml |
1ml |
现货  |
|
| 别名 | 多拉马莫德 (BIRB 796) |
|---|---|
| 英文别名 | 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Doramapimod (BIRB 796) |
| 生化机理 | 多拉帕莫德（BIRB 796）是一种泛 p38 MAPK 抑制剂，在无细胞实验中对 p38α/β/γ/δ 的 IC50 值分别为 38 nM、65 nM、200 nM 和 520 nM，在 THP-1 细胞中与 p38α 结合的Kd值为 0.1 nM，对 JNK2 的选择性高 330 倍，对 c-RAF、Fyn 和 Lck 的抑制作用较弱，对 ERK-1、SYK、IKK2 的抑制作用不明显。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | MAP 激酶 p38 alpha 抑制剂 |
| 产品介绍 |
BIRB 796 (Doramapimod)是一种高度选择性的p38α MAPK抑制剂，Kd为0.1 nM，比作用于JNK2选择性高330倍，微弱抑制c-RAF， Fyn和Lck，也微弱抑制ERK-1， SYK， IKK2， ZAP-70， EGFR， HER2， PKA， PKC， PKCα/β/γ。A p38α MAPK and JNK2 Information Doramapimod (BIRB 796) is a pan-p38 MAPKinhibitor withIC50of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and bindsp38αwithKdof 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, BIRB 796 shows no significant inhibition to ERK-1, SYK, IKK2β, ZAP-70, EGF receptor kinase, HER2, protein kinase A (PKA), PKC, PKC-α, PKC-β (I and II) and PKC-γ. BIRB 796 greatly improves binding affinity by forming a hydrogen bond between the morpholine oxygen and the ATP-binding domain of p38α. BIRB 796 represents one of the most potent and slowest dissociating inhibitors against human p38 MAP kinase now known. BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively. BIRB796 also inhibits the activity and the activation of SAPK3/p38γ at a higher concentration than it does in p38α. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97, which is a physiological substrate of SAPK3/p38γ. BIRB796 blocks JNK1/2 activation and activity in HEK293 cells, while not inhibits the activation and activity of ERK1/ERK2 in Hela cells. Moreover, the binding of BIRB796 to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4 rather than enhancing their dephosphorylation. BIRB 796 blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation, thereby enhancing cytotoxicity and caspase activation. BIRB 796 downregulates IL-6 and VEGF secretion in BMSCs triggered by TNF-α and TGF-β1. BIRB-796 has a pyrazole scaffold that places a lipophilic t-butyl group into the lower selectivity site and a tolyl ring into the upper selectivity site. BIRB-796 also inhibits B-Raf and Abl with IC50 of 83\xa0nM and 14.6\xa0μM, respectively. In vivo BIRB 796 (30 mg/kg) inhibits 84% of TNF-α in LPS-stimulated mice and demonstrates efficacy in a mouse model of established collagen-induced arthritis. BIRB 796 has good pharmacokinetic performance even after oral administration in mice. cell lines： Concentrations： Incubation Time： Powder Purity:≥98% |
| ALogP | 5.7 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5 |
| 分子量 | 527.67 |
| Reaxy-Rn | 9170597 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9170597&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 71 mg/mL (199.23 mM); Water: 71 mg/mL (199.23 mM); Ethanol: 1 mg/mL (2.8 mM); |
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