Doramapimod (BIRB 796)

製品コードS1574

Doramapimod (BIRB 796)化学構造

分子量(MW):527.66

Doramapimod (BIRB 796)は一種のpan-p38 MAPK阻害剤で、無細胞試験でp38α/β/γ/δに作用する時のIC50値が38 nM、65 nM、200 nM と520 nMにそれぞれ分かれることですが、p38αと結合することができて、THP-1細胞の中にこのKd値が0.1 nMになって、p38α/β/γ/δに作用する選択性はJNK2に作用する選択性より330倍が高くなって、c-RAF、Fyn とLckに少し弱い抑制作用を表して、ERK-1、SYKとIKK2にも微弱な抑制作用を表します。

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カスタマーフィードバック(5)

  • 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.

    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.

  • 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.

    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.

製品安全説明書

p38 MAPK阻害剤の選択性比較

生物活性

製品説明 Doramapimod (BIRB 796)は一種のpan-p38 MAPK阻害剤で、無細胞試験でp38α/β/γ/δに作用する時のIC50値が38 nM、65 nM、200 nM と520 nMにそれぞれ分かれることですが、p38αと結合することができて、THP-1細胞の中にこのKd値が0.1 nMになって、p38α/β/γ/δに作用する選択性はJNK2に作用する選択性より330倍が高くなって、c-RAF、Fyn とLckに少し弱い抑制作用を表して、ERK-1、SYKとIKK2にも微弱な抑制作用を表します。
特性 The first p38 MAPK inhibitor to be tested in a phase III clinical trial.
ターゲット
p38α [1]
(Cell-free assay)
p38α [7]
0.1 nM(Kd) 38 nM
体外試験

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. [1] BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively. [2] 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. [3] 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. [4] 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 nM and 14.6 μM, respectively. [5]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell M1L3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL4UI5OUUN3ME2wMlM1PzZ|IN88US=> NVTBc45tW0GQR2LFVi=>
DU-145 NGjCcZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNwOUO4NVEh|ryP MVLTRW5IWkWU
GOTO NI\uOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTZwM{mxOlEh|ryP MWTTRW5IWkWU
NCI-H358 NFK0T3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L6cWlEPTB;Nz61N|gh|ryP MnHUV2FPT1KHUh?=
IST-MES1 NEHTUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTdwOUW2N|ch|ryP M{[2VXNCVkeURWK=
KP-N-YN NWT1ZlFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLLeFFKSzVyPUiuNlAyQSEQvF2= Ml;SV2FPT1KHUh?=
T-24 MnnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfwW4JTUUN3ME24MlQxPjd|IN88US=> MYPTRW5IWkWU
MPP-89 NFW3WWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW5TWM2OD16LkS2NlUyKM7:TR?= NYfj[4tRW0GQR2LFVi=>
NCI-SNU-1 M4rURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fBWmlEPTB;OT6wOlc{QSEQvF2= MYTTRW5IWkWU
BFTC-905 M{izN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPzTWM2OD1zMD6xNlM{KM7:TR?= MmP1V2FPT1KHUh?=
MS-1 M{W3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFyLkiyN|Uh|ryP MVXTRW5IWkWU
NBsusSR M2D6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEOxXohKSzVyPUGwMlgzOzVizszN MkG3V2FPT1KHUh?=
BEN MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17ybmlEPTB;MUOuNVI3PCEQvF2= M17yXXNCVkeURWK=
HMV-II NYTTfVh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT2TWM2OD1zND6yN|A6KM7:TR?= Mn21V2FPT1KHUh?=
NCI-H1581 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnnR21KSzVyPUG3MlA1PDdizszN Ml7qV2FPT1KHUh?=
ES8 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF5LkG2O{DPxE1? M1\GUXNCVkeURWK=
LC-2-ad MmnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTF5LkSzOlYh|ryP MoG5V2FPT1KHUh?=
EW-13 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVi5bIttUUN3ME2xO{46PTF4IN88US=> M4rXc3NCVkeURWK=
AN3-CA Mn\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq2eWVKSzVyPUG4MlEh|ryP NHTxfndUSU6JUlXS
DB NXvDbY9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF6Lke5NlMh|ryP NHz5O3NUSU6JUlXS
SK-MEL-1 NV:5c2tGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJyLkO2PFMh|ryP MkHVV2FPT1KHUh?=
CAPAN-1 NYPtcJNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn1O3JSUUN3ME2yNk4yQDh2IN88US=> M3y5fHNCVkeURWK=
NCI-H2228 NVXGVZd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;0TIF2UUN3ME2yN{43PjZ6IN88US=> NYf3emF7W0GQR2LFVi=>
HOP-92 NG\1S|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;nTWM2OD1{ND6zPFM5KM7:TR?= NXXlZoRPW0GQR2LFVi=>
KYSE-270 M4O2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofETWM2OD1{ND61OVc{KM7:TR?= MlzuV2FPT1KHUh?=
HCC1806 MmrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPkc2ZKSzVyPUK0Mlc4QTlizszN MWnTRW5IWkWU
HuO-3N1 NUThR2dFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\kVWlEPTB;MkWuPFE5PSEQvF2= M{Cxe3NCVkeURWK=
HOS M4DZbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi0fYkxUUN3ME2yOU46Ojl{IN88US=> M3HCenNCVkeURWK=
KYSE-510 Moj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TsSGlEPTB;Mk[uNVYyOiEQvF2= MVnTRW5IWkWU
COLO-741 NGDLXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH2TWM2OD1{Nj6zN|I6KM7:TR?= MYfTRW5IWkWU
H-EMC-SS NWrqfpY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJ4LkmyOFUh|ryP NVPnOXBEW0GQR2LFVi=>
HCC1937 M3v3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jiOWlEPTB;MkeuNlI{QCEQvF2= NYHEfnNDW0GQR2LFVi=>
NCI-H2126 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJ5LkO5O|Uh|ryP MYDTRW5IWkWU
NCI-H1703 MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm4TWM2OD1{OD6wOFE{KM7:TR?= MlzkV2FPT1KHUh?=
U-2-OS M4H3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvpTWM2OD1{OD61OVE2KM7:TR?= NIflRXRUSU6JUlXS
DBTRG-05MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HQWGlEPTB;MkiuOVY2OSEQvF2= NVn3R4ttW0GQR2LFVi=>
MHH-ES-1 NHPYWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXmdllCUUN3ME2zNU46PDFizszN MUDTRW5IWkWU
HCC1419 NYK3WJlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmzTWM2OD1|Mj6xNVE6KM7:TR?= NYD6c5VoW0GQR2LFVi=>
HOP-62 NVOwcpR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fjZWlEPTB;M{KuNlcxOSEQvF2= MnLEV2FPT1KHUh?=
AM-38 M1TuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\BfZNKSzVyPUOyMlk6OzFizszN MnLXV2FPT1KHUh?=
NCI-H2009 M3rvOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnEVnBKSzVyPUOzMlQxODdizszN NWX0RZo{W0GQR2LFVi=>
EM-2 NHfnNoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT4T3dDUUN3ME2zN{42PTFzIN88US=> NFzU[VhUSU6JUlXS
SW1116 MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTFdVZKSzVyPUO0MlQ5OzhizszN NVu2TVJ6W0GQR2LFVi=>
SK-N-AS NF7tb3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfNe3FKSzVyPUO1MlA4OTRizszN NIDaOGJUSU6JUlXS
ChaGo-K-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi0WYh7UUN3ME2zOU43ODN{IN88US=> M2j2XnNCVkeURWK=
RT-112 M1rqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfjTWM2OD1|NT65PFc6KM7:TR?= Mny0V2FPT1KHUh?=
HTC-C3 NXLMXWlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vPVWlEPTB;M{[uNlM2PSEQvF2= NYLJVY12W0GQR2LFVi=>
SK-NEP-1 NYXBVZpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqyOGY1UUN3ME2zOk43OTB4IN88US=> MXLTRW5IWkWU
LB831-BLC MonnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DYeGlEPTB;M{euOlU1OSEQvF2= MXfTRW5IWkWU
CTB-1 NYH0SW9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTN6LkS1NVIh|ryP NX3ZNnFKW0GQR2LFVi=>
MOLT-4 MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTN6LkizPVEh|ryP MVXTRW5IWkWU
SW756 M1LZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPqTWM2OD12MD65N|g2KM7:TR?= MUXTRW5IWkWU
CAL-72 NVn2botjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXHTWM2OD12Mj6wN{DPxE1? M{SzWnNCVkeURWK=
KNS-62 MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37M[2lEPTB;NEKuOlI6PiEQvF2= NUDubolWW0GQR2LFVi=>
KARPAS-299 MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm3UplHUUN3ME20N{4{OjN|IN88US=> NGW5c2xUSU6JUlXS
HEL MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDBTWM2OD12NT60OlQ3KM7:TR?= MUHTRW5IWkWU
KP-4 M3q1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7SU3hKSzVyPUS2Mlc{PjFizszN M1yxV3NCVkeURWK=
NEC8 Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3YTWM2OD12Nz6xOlYyKM7:TR?= MXLTRW5IWkWU
G-402 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFWzO2dKSzVyPUS4MlcxOTJizszN MUTTRW5IWkWU

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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. [1] BIRB 796 has good pharmacokinetic performance even after oral administration in mice. [2]

お薦めの試験操作(参考用のみ)

動物試験:

[2]

+ 展開
  • 動物モデル: Collagen-induced arthritis in female Balb/c mice
  • 製剤: 70% PEG400 (intravenous) or 100% PEG400 (oral)
  • 投薬量: 1 mg/kg (intravenous) or 10 mg/kg (oral)
  • 投与方法: Intravenous injection or by oral
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 106 mg/mL (200.88 mM)
Ethanol 106 mg/mL (200.88 mM)
Water slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 527.66
化学式

C31H37N5O3

CAS No. 285983-48-4
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02214888 Terminated Arthritis, Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209805 Completed Healthy Boehringer Ingelheim January 2001 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

p38 MAPK信号経路図

p38 MAPK Inhibitors with Unique Features

相関p38 MAPK製品

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID