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。

サイズ 価格(税別) 在庫  
JPY 48804.00 あり
JPY 24402.00 あり
JPY 44820.00 あり
JPY 78020.00 あり

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 NWezPHBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLKTWM2OD1yLkO0O|Y{KM7:TR?= NXnuV|c4W0GQR2LFVi=>
DU-145 M4XrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW4TWM2OD1|LkmzPFEyKM7:TR?= MWfTRW5IWkWU
GOTO MlvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzIdpBLUUN3ME22MlM6OTZzIN88US=> NUK5Um42W0GQR2LFVi=>
NCI-H358 NFrmXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTdwNUO4JO69VQ>? NVvuc|R{W0GQR2LFVi=>
IST-MES1 NUT4[XlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrpRXJKSzVyPUeuPVU3OzdizszN MYXTRW5IWkWU
KP-N-YN MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmzSlBKSzVyPUiuNlAyQSEQvF2= NGHPc2RUSU6JUlXS
T-24 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3j4bWlEPTB;OD60NFY4OyEQvF2= MVjTRW5IWkWU
MPP-89 M1;hcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXUbFZGUUN3ME24MlQ3OjVzIN88US=> M3r4dnNCVkeURWK=
NCI-SNU-1 MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n4ZWlEPTB;OT6wOlc{QSEQvF2= MmDQV2FPT1KHUh?=
BFTC-905 M3\Vdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mom1TWM2OD1zMD6xNlM{KM7:TR?= MYXTRW5IWkWU
MS-1 NET2XmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLYbZhKSzVyPUGwMlgzOzVizszN NVO2[HJUW0GQR2LFVi=>
NBsusSR M4ThdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HpSWlEPTB;MUCuPFI{PSEQvF2= M3XsSnNCVkeURWK=
BEN MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q5XmlEPTB;MUOuNVI3PCEQvF2= MUXTRW5IWkWU
HMV-II MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTF2LkKzNFkh|ryP M1XGTXNCVkeURWK=
NCI-H1581 NWn2UYVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHlOHlVUUN3ME2xO{4xPDR5IN88US=> Mny2V2FPT1KHUh?=
ES8 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvnUWNlUUN3ME2xO{4yPjdizszN NH3senJUSU6JUlXS
LC-2-ad MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF5LkSzOlYh|ryP M12zWHNCVkeURWK=
EW-13 NVnLTVNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q2cGlEPTB;MUeuPVUyPiEQvF2= NWK3TYp4W0GQR2LFVi=>
AN3-CA NXjMR2p2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv4fZdKSzVyPUG4MlEh|ryP NV3vcG55W0GQR2LFVi=>
DB NWDZN|MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TWWmlEPTB;MUiuO|kzOyEQvF2= MnW4V2FPT1KHUh?=
SK-MEL-1 M2\SW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu3cHlJUUN3ME2yNE4{Pjh|IN88US=> NET0eZVUSU6JUlXS
CAPAN-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fUfWlEPTB;MkKuNVg5PCEQvF2= NX3m[|ZEW0GQR2LFVi=>
NCI-H2228 NX7xflhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\iWG1KSzVyPUKzMlY3PjhizszN MXzTRW5IWkWU
HOP-92 NI\UTo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTJ2LkO4N|gh|ryP M3fHR3NCVkeURWK=
KYSE-270 M4PRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvxbZVJUUN3ME2yOE42PTd|IN88US=> NEnuSVlUSU6JUlXS
HCC1806 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\0TWM2OD1{ND63O|k6KM7:TR?= Mny3V2FPT1KHUh?=
HuO-3N1 NH\1c45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LhV2lEPTB;MkWuPFE5PSEQvF2= MlP0V2FPT1KHUh?=
HOS M1\XWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITTboJKSzVyPUK1MlkzQTJizszN M1\KWnNCVkeURWK=
KYSE-510 NEfsXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PjfWlEPTB;Mk[uNVYyOiEQvF2= M1TSVXNCVkeURWK=
COLO-741 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzHb5RnUUN3ME2yOk4{OzJ7IN88US=> NGeweGJUSU6JUlXS
H-EMC-SS Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnLOoJKSzVyPUK2MlkzPDVizszN MWnTRW5IWkWU
HCC1937 NVT0OZhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7Zbos{UUN3ME2yO{4zOjN6IN88US=> MVzTRW5IWkWU
NCI-H2126 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\NTo9KSzVyPUK3MlM6PzVizszN NIrlNFdUSU6JUlXS
NCI-H1703 NV\GVoE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17uNWlEPTB;MkiuNFQyOyEQvF2= NGOxVWhUSU6JUlXS
U-2-OS MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX2zOFFrUUN3ME2yPE42PTF3IN88US=> M2PidXNCVkeURWK=
DBTRG-05MG NYP1NFczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvPR|dKSzVyPUK4MlU3PTFizszN MYnTRW5IWkWU
MHH-ES-1 M16zUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTNzLkm0NUDPxE1? MXnTRW5IWkWU
HCC1419 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTN{LkGxNVkh|ryP NH\YbopUSU6JUlXS
HOP-62 NYfyZoxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTN{LkK3NFEh|ryP MVrTRW5IWkWU
AM-38 NH\6WZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X2WWlEPTB;M{KuPVk{OSEQvF2= NVrsSmdvW0GQR2LFVi=>
NCI-H2009 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTN|LkSwNFch|ryP Moi3V2FPT1KHUh?=
EM-2 M3y5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\ITWM2OD1|Mz61OVEyKM7:TR?= MlvEV2FPT1KHUh?=
SW1116 Ml65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTN2LkS4N|gh|ryP MUfTRW5IWkWU
SK-N-AS NVXwfnhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP1dG1KSzVyPUO1MlA4OTRizszN Mn\sV2FPT1KHUh?=
ChaGo-K-1 NYTWWllwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rXbmlEPTB;M{WuOlA{OiEQvF2= M1P4b3NCVkeURWK=
RT-112 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37zXmlEPTB;M{WuPVg4QSEQvF2= NF:3eXVUSU6JUlXS
HTC-C3 M2fmOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDRPWdpUUN3ME2zOk4zOzV3IN88US=> MoHKV2FPT1KHUh?=
SK-NEP-1 NF7jeZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3uy[GlEPTB;M{[uOlExPiEQvF2= NYC2OFBpW0GQR2LFVi=>
LB831-BLC NF\2cHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvWZZJKSzVyPUO3MlY2PDFizszN MmPGV2FPT1KHUh?=
CTB-1 M1fzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkGxTWM2OD1|OD60OVEzKM7:TR?= M1zRUXNCVkeURWK=
MOLT-4 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN6LkizPVEh|ryP NX;WR25RW0GQR2LFVi=>
SW756 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknlTWM2OD12MD65N|g2KM7:TR?= NWX5Smp{W0GQR2LFVi=>
CAL-72 NIPrcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLheoF3UUN3ME20Nk4xOyEQvF2= NH3yR5VUSU6JUlXS
KNS-62 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PHfWlEPTB;NEKuOlI6PiEQvF2= NYm0V294W0GQR2LFVi=>
KARPAS-299 NFzifVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jj[2lEPTB;NEOuN|I{OyEQvF2= MkLPV2FPT1KHUh?=
HEL NHTaW3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHRXolKSzVyPUS1MlQ3PDZizszN NHPHSZVUSU6JUlXS
KP-4 NGDiXIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTxfVhKSzVyPUS2Mlc{PjFizszN NUXyTFNLW0GQR2LFVi=>
NEC8 MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXkTWM2OD12Nz6xOlYyKM7:TR?= M{D2dnNCVkeURWK=
G-402 NVL5OINWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTR6LkewNVIh|ryP M13lenNCVkeURWK=

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 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
Water 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
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