Doramapimod (BIRB 796)

目录号:S1574

Doramapimod (BIRB 796) Chemical Structure

Molecular Weight(MW): 527.66

Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂,在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM,65 nM,200 nM 和520 nM,并且能够与p38α结合,在THP-1细胞中Kd为0.1 nM,比作用于JNK2选择性高330倍,对c-RAF,Fyn 和Lck具有较弱的抑制作用,对ERK-1,SYK,IKK2也有微弱抑制作用。

规格 价格 库存 购买数量  
RMB 2403.35 现货
RMB 1221.86 现货
RMB 2215.96 现货
RMB 3866.11 现货
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客户使用Selleck该产品发表文献18篇:

客户使用该产品的5个实验数据:

  • Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.

    Blood 2012 119(26), 6255-8. Doramapimod (BIRB 796) purchased from Selleck.

    Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.

    Int J Cancer 2014 134(3), 575-86. Doramapimod (BIRB 796) purchased from Selleck.

  • A p38α/ERK crosstalk exists in CRC cells and tissues. Use of a structurally and functionally different p38α inhibitor (BIRB-796) confirms ERK1/2 phospho-activation. Using BIRB-796 for up to 72 h triggers MEK-ERK1/2 signaling in HT-29 cells.

    Cancer Lett 2012 324(1), 98-108. Doramapimod (BIRB 796) purchased from Selleck.

    Inhibition of p38 MAPK activity prevents induction of autophagy by glucose. NIH 3T3 cells were incubated in KH medium without glucose in the presence of the p38 MAPK inhibitor BIRB796 (50 nM, middle panels). After 30 min, glucose (10 mM) and lysosomal inhibitors were added to the indicated samples and cells were further incubated for 2 h. Cell lysates were collected and processed for SDS/PAGE. LC3 levels were detected and actin served as a loading control. The values shown in the histograms represent means盨.D. from three independent experiments with the LC3-II levels normalized to actin and expressed as a percentage of the values of KH medium without glucose. *P<0.05. Glc, glucose; w/o, without.

    Biochem J 2014 449(2), 497-506. Doramapimod (BIRB 796) purchased from Selleck.

  • Doramapimod (BIRB 796) purchased from Selleck.

产品安全说明书

p38 MAPK抑制剂选择性比较

生物活性

产品描述 Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂,在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM,65 nM,200 nM 和520 nM,并且能够与p38α结合,在THP-1细胞中Kd为0.1 nM,比作用于JNK2选择性高330倍,对c-RAF,Fyn 和Lck具有较弱的抑制作用,对ERK-1,SYK,IKK2也有微弱抑制作用。
特性 BIRB 796是第一个进入三期临床试验的p38 MAPK抑制剂。
靶点
p38α [1]
(Cell-free assay)
p38α [7]
0.1 nM(Kd) 38 nM
体外研究

BIRB 796作用于ERK-1,SYK,IKK2β,ZAP-70,EGFR激酶,HER2,蛋白激酶 A(PKA),PKC,PKC-α,PKC-β(I和II)和PKC-γ没有明显抑制效果。BIRB 796通过在吗啉氧和p38α的ATP结合域间形成氢键,显著提高亲和力。BIRB 796是作用于人类p38 MAPK的最有效和分离最慢的抑制剂之一。[1] BIRB 796 有效抑制c-Raf-1和Jnk2α2,IC50分别为1.4和0.1 nM。[2] 高浓度BIRB796也抑制SAPK3/p38γ的活性和激活。BIRB796阻断压力诱导的框架蛋白SAP97磷酸化, SAP97是SAPK3/p38γ的底物。BIRB796作用于HEK293细胞,阻断JNK1/2激活和活性,而作用于Hela细胞,不抑制ERK1/ERK2激活和活性。而且, BIRB796与p38 MAPKs或JNK1/2的结合,降低上游激酶MKK6或MKK4磷酸化,而不增强去磷酸化。 [3] BIRB 796 作用于TNF-α和TGF-β1引起的BMSCs,下调IL-6和VEGF分泌。[4] BIRB-796有吡唑环 ,使亲脂的末端异丁基基团 与低选择性位点结合,甲苯基环与高选择性位点结合。BIRB-796也抑制B-Raf和Abl,IC50分别为83 nM 和14.6 μM。 [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NI\0O3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnZSWVKSzVyPUCuN|Q4PjNizszN NGX5[|RUSU6JUlXS
DU-145 Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDNTWM2OD1|LkmzPFEyKM7:TR?= M2i0PHNCVkeURWK=
GOTO NV;kclhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn70TWM2OD14LkO5NVYyKM7:TR?= M{OxRXNCVkeURWK=
NCI-H358 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzHcW1QUUN3ME23MlU{QCEQvF2= NFTJeo5USU6JUlXS
IST-MES1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfJTWM2OD15Lkm1OlM4KM7:TR?= Ml[3V2FPT1KHUh?=
KP-N-YN NHXiVmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRThwMkCxPUDPxE1? NVfVV4RFW0GQR2LFVi=>
T-24 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRThwNEC2O|Mh|ryP MW\TRW5IWkWU
MPP-89 MoXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLJTWM2OD16LkS2NlUyKM7:TR?= MmTKV2FPT1KHUh?=
NCI-SNU-1 NIXPUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfwRXdKSzVyPUmuNFY4OzlizszN Mn63V2FPT1KHUh?=
BFTC-905 M{XW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfoTFBKSzVyPUGwMlEzOzNizszN NUXLbnBYW0GQR2LFVi=>
MS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLmdJRpUUN3ME2xNE45OjN3IN88US=> NGf0WYtUSU6JUlXS
NBsusSR M3ftdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFyLkiyN|Uh|ryP NVv5VYcyW0GQR2LFVi=>
BEN MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDEWmNKSzVyPUGzMlEzPjRizszN M{KwSXNCVkeURWK=
HMV-II NGj2cnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPOTWM2OD1zND6yN|A6KM7:TR?= MlvhV2FPT1KHUh?=
NCI-H1581 M{DE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF5LkC0OFch|ryP NFjDO5RUSU6JUlXS
ES8 M3fkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrVTWM2OD1zNz6xOlch|ryP NWL0UIw5W0GQR2LFVi=>
LC-2-ad NH7KVZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XRPWlEPTB;MUeuOFM3PiEQvF2= MUHTRW5IWkWU
EW-13 M4rMZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTF5Lkm1NVYh|ryP MULTRW5IWkWU
AN3-CA M4q1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;rTplKSzVyPUG4MlEh|ryP NX3aW|NiW0GQR2LFVi=>
DB Mnr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTtNGhKSzVyPUG4Mlc6OjNizszN NVLwVmliW0GQR2LFVi=>
SK-MEL-1 MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJyLkO2PFMh|ryP MVLTRW5IWkWU
CAPAN-1 M3HINWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv0d4RKSzVyPUKyMlE5QDRizszN NXSzZYJ3W0GQR2LFVi=>
NCI-H2228 MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzWWFdOUUN3ME2yN{43PjZ6IN88US=> Mn\vV2FPT1KHUh?=
HOP-92 M{fKdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ2LkO4N|gh|ryP NY\aUVdPW0GQR2LFVi=>
KYSE-270 M3\Q[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPDWWZKSzVyPUK0MlU2PzNizszN NWi5NJBWW0GQR2LFVi=>
HCC1806 NWraNWNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnewTWM2OD1{ND63O|k6KM7:TR?= MV;TRW5IWkWU
HuO-3N1 NHrQUHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ3LkixPFUh|ryP M37TfHNCVkeURWK=
HOS NYS0dHpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7TXVlKSzVyPUK1MlkzQTJizszN NVHJcGJXW0GQR2LFVi=>
KYSE-510 NYjUPFU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK5dnNKSzVyPUK2MlE3OTJizszN NXfxbGJ2W0GQR2LFVi=>
COLO-741 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml23TWM2OD1{Nj6zN|I6KM7:TR?= NU\iPIZmW0GQR2LFVi=>
H-EMC-SS NGfO[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrZb4x1UUN3ME2yOk46OjR3IN88US=> M1fwVXNCVkeURWK=
HCC1937 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJ5LkKyN|gh|ryP MkS4V2FPT1KHUh?=
NCI-H2126 M3LsVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzDSnRKSzVyPUK3MlM6PzVizszN MlnjV2FPT1KHUh?=
NCI-H1703 M3WxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJ6LkC0NVMh|ryP MXLTRW5IWkWU
U-2-OS M1nuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LsN2lEPTB;MkiuOVUyPSEQvF2= MYDTRW5IWkWU
DBTRG-05MG M3z1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ6LkW2OVEh|ryP M4fkZ3NCVkeURWK=
MHH-ES-1 M2r2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTNzLkm0NUDPxE1? NVXweI01W0GQR2LFVi=>
HCC1419 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPWVJFKSzVyPUOyMlEyOTlizszN NHW5XGJUSU6JUlXS
HOP-62 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vibGlEPTB;M{KuNlcxOSEQvF2= NYHqbJZQW0GQR2LFVi=>
AM-38 M{\zWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jDWGlEPTB;M{KuPVk{OSEQvF2= M4HMbXNCVkeURWK=
NCI-H2009 NVrrVVFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;STWM2OD1|Mz60NFA4KM7:TR?= NHrkTmJUSU6JUlXS
EM-2 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTN|LkW1NVEh|ryP M{XoTXNCVkeURWK=
SW1116 M2\5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXsSm9WUUN3ME2zOE41QDN6IN88US=> MnLVV2FPT1KHUh?=
SK-N-AS MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\td2dpUUN3ME2zOU4xPzF2IN88US=> MWHTRW5IWkWU
ChaGo-K-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzHNVNKSzVyPUO1MlYxOzJizszN M1K3VXNCVkeURWK=
RT-112 M1zxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzPTWM2OD1|NT65PFc6KM7:TR?= MWrTRW5IWkWU
HTC-C3 M2C2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTN4LkKzOVUh|ryP NEXtW4VUSU6JUlXS
SK-NEP-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XzVGlEPTB;M{[uOlExPiEQvF2= M4LReXNCVkeURWK=
LB831-BLC M1z0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjLc4dKSzVyPUO3MlY2PDFizszN MU\TRW5IWkWU
CTB-1 NX22dlY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DMXmlEPTB;M{iuOFUyOiEQvF2= MoLSV2FPT1KHUh?=
MOLT-4 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\LO4xKSzVyPUO4Mlg{QTFizszN NFP0b5ZUSU6JUlXS
SW756 MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnUTWM2OD12MD65N|g2KM7:TR?= MnLSV2FPT1KHUh?=
CAL-72 NX\3NZEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL4TWM2OD12Mj6wN{DPxE1? M4W2fnNCVkeURWK=
KNS-62 M4\ZbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknrTWM2OD12Mj62Nlk3KM7:TR?= MVvTRW5IWkWU
KARPAS-299 NVXNd|E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR|LkOyN|Mh|ryP M2XNXHNCVkeURWK=
HEL NUX0b5BLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\CTWM2OD12NT60OlQ3KM7:TR?= NE\nT29USU6JUlXS
KP-4 NHXMeZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR4LkezOlEh|ryP Mn2wV2FPT1KHUh?=
NEC8 M4\PdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYewUIRPUUN3ME20O{4yPjZzIN88US=> M1vPNXNCVkeURWK=
G-402 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTqU5pKSzVyPUS4MlcxOTJizszN NIXxe5lUSU6JUlXS

... Click to View More Cell Line Experimental Data

体内研究 BIRB 796按30 mg/kg剂量作用于LPS刺激的鼠,抑制TNF-α达84%。作用于患胶原诱导的关节炎鼠显示高效性。[1] BIRB 796口服处理给鼠,具有好的药物动力学特征。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:

[2]

+ 展开
  • Animal Models: 患胶原诱导的关节炎雌性Balb/c鼠
  • Formulation: 70% PEG400(静脉注射)或100% PEG400(口服)
  • Dosages: 1 mg/kg(静脉注射)或10 mg/kg(口服)
  • Administration: 静脉注射或口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 527.66
化学式

C31H37N5O3

CAS号 285983-48-4
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02214888 Terminated Arthritis Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02214888 Terminated Arthritis Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2

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操作手册

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p38 MAPK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID