计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
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,
In vitro
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 Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
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。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
MAP 激酶 p38 alpha 抑制剂
名称和识别符
EC号
111-112-5
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=
技术文档
高级数据
产品属性
| ALogP | 5.7 |
|---|
关联靶点（人）
DDR2
Tchem
含盘状结构域受体 2(Discoidin domain-containing receptor 2)
(3 活性数据)
DDR1
Tchem
上皮盘状结构域受体 1(Epithelial discoidin domain-containing receptor 1)
(3 活性数据)
STK10
Tchem
丝氨酸/苏氨酸蛋白激酶10(Serine/threonine-protein kinase 10)
(3 活性数据)
ABCB1
Tchem
多药耐药蛋白1(Multidrug resistance protein 1)
(1 活性数据)
HSPB1
Tchem
热休克蛋白β-1(Heat shock protein beta-1)
(1 活性数据)
TNF
Tclin
肿瘤坏死因子(Tumor necrosis factor)
(2 活性数据)
TNIK
Tchem
TRAF2 与 NCK 相互作用蛋白激酶(TRAF2 and NCK-interacting protein kinase)
(1 活性数据)
TEK
Tclin
血管生成素-1受体(Angiopoietin-1 receptor)
(4 活性数据)
MAPK12
Tchem
丝裂原活化蛋白激酶 12(Mitogen-activated protein kinase 12)
(4 活性数据)
TIE1
Tchem
酪氨酸蛋白激酶受体 Tie-1(Tyrosine-protein kinase receptor Tie-1)
(2 活性数据)
MAPK9
Tchem
丝裂原活化蛋白激酶9(Mitogen-activated protein kinase 9)
(9 活性数据)
MAPK11
Tchem
丝裂原活化蛋白激酶 11(Mitogen-activated protein kinase 11)
(3 活性数据)
MAPK13
Tchem
丝裂原活化蛋白激酶 13(Mitogen-activated protein kinase 13)
(1 活性数据)
MAPK14
Tchem
丝裂原活化蛋白激酶 14(Mitogen-activated protein kinase 14)
(33 活性数据)
化学和物理性质
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);
安全和危险性（GHS）
信号词
警告
危险声明
H302: 吞食有害
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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