Doramapimod (BIRB 796)

Name: Doramapimod (BIRB 796)
Brand: Selleck Chemicals
SKU: S1574
Rating: 5 (82 reviews)

For research use only.

Catalog No.S1574

82 publications

Doramapimod (BIRB 796) Chemical Structure

CAS No. 285983-48-4

Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

Selleck's Doramapimod (BIRB 796) has been cited by 82 publications

Nature, 2020, 3

PubMed: 32494007 ( click the link to review the publication )

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Nat Chem Biol, 2013, 9(7):428-36

PubMed: 23685672 ( click the link to review the publication )

Mol Immunol, 2021, 133:135-145

PubMed: 33662817 ( click the link to review the publication )

Exp Ther Med, 2021, 21(5):440

PubMed: 33747177 ( click the link to review the publication )

J Mol Med (Berl), 2021, 10.1007/s00109-021-02046-6

PubMed: 33575853 ( click the link to review the publication )

Genome Biol, 2020, 21(1):33

PubMed: 32039742 ( click the link to review the publication )

J Clin Invest, 2020, 130(3):1377-1391

PubMed: 31877112 ( click the link to review the publication )

Elife, 2020, 9e60541

PubMed: 32940599 ( click the link to review the publication )

Redox Biol, 2020, 28:101445

PubMed: 32037305 ( click the link to review the publication )

Cancers (Basel), 2020, 10;12(6):E1516

PubMed: 32531927 ( click the link to review the publication )

Cells, 2020, 17;9(4) pii: E1003

PubMed: 32316635 ( click the link to review the publication )

Mol Oncol, 2020, 10.1002/1878-0261.12882

PubMed: 33320980 ( click the link to review the publication )

J Cell Mol Med, 2020, 10.1111/jcmm.16223

PubMed: 33345444 ( click the link to review the publication )

Cell Immunol, 2020, 347:104027

PubMed: 31864664 ( click the link to review the publication )

J Vet Intern Med, 2020, 10.1111/jvim.15847

PubMed: 32700419 ( click the link to review the publication )

J Hepatol, 2019, 71(1):163-174

PubMed: 30914267 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2387

PubMed: 31160572 ( click the link to review the publication )

Redox Biol, 2019, 21:101061

PubMed: 30590310 ( click the link to review the publication )

Arterioscler Thromb Vasc Biol, 2019, 39(12):e253-e272

PubMed: 31578081 ( click the link to review the publication )

Cell Death Discov, 2019, 5:104

PubMed: 31240131 ( click the link to review the publication )

Oncoimmunology, 2019,

PubMed: 31143512 ( click the link to review the publication )

Mol Oncol, 2019, 13(2):264-289

PubMed: 30422386 ( click the link to review the publication )

Pharmacol Res, 2019, 143:73-85

PubMed: 30862605 ( click the link to review the publication )
Antiviral Res, 2019, 170:104572

PubMed: 31376425 ( click the link to review the publication )

Neurogastroenterol Motil, 2019, 31(6):e13555

PubMed: 30793435 ( click the link to review the publication )

Life Sci, 2019, 10.1016/j.lfs.2019.116583

PubMed: 31226417 ( click the link to review the publication )

J Cancer Res Clin Oncol, 2019, 145(2):411-427

PubMed: 30483898 ( click the link to review the publication )

Eur J Pharmacol, 2019, 865:172760

PubMed: 31669588 ( click the link to review the publication )

J Allergy Clin Immunol, 2019, 144(4):1036-1049

PubMed: 31378305 ( click the link to review the publication )

Blood, 2018, 131(11):1219-1233

PubMed: 29288170 ( click the link to review the publication )

J Clin Invest, 2018, 128(10):4485-4500

PubMed: 30024858 ( click the link to review the publication )

Aging Cell, 2018, 17(1)

PubMed: 29024417 ( click the link to review the publication )

Elife, 2018, 7

PubMed: 29595474 ( click the link to review the publication )

Sci Signal, 2018,

PubMed: 29511118 ( click the link to review the publication )

PLoS Genet, 2018, 14(9):e1007621

PubMed: 30222786 ( click the link to review the publication )

Sci Rep, 2018, 8(1):5007

PubMed: 29568068 ( click the link to review the publication )

Invest Ophthalmol Vis Sci, 2018, 59(10):4218-4227

PubMed: 30128493 ( click the link to review the publication )

Biochemistry, 2018, 57(48):6715-6725

PubMed: 30418016 ( click the link to review the publication )

Mol Cell Biol, 2018, 38(11)e00647-17

PubMed: 29530922 ( click the link to review the publication )

Oncotarget, 2018, 9(51):29680-29697

PubMed: 30038713 ( click the link to review the publication )

J Clin Invest, 2017, 127(9):3339-3352

PubMed: 28758906 ( click the link to review the publication )

Cell Death Dis, 2017, 8(8):e2967

PubMed: 28771230 ( click the link to review the publication )

J Mol Cell Biol, 2017, 1;9(2):154-165

PubMed: 27927748 ( click the link to review the publication )

Stem Cells, 2017, 35(4):909-919

PubMed: 28248004 ( click the link to review the publication )

Front Immunol, 2017, 8:818

PubMed: 28769928 ( click the link to review the publication )

Mol Neurobiol, 2017, 54(10):7597-7609

PubMed: 27832521 ( click the link to review the publication )

J Cell Commun Signal, 2017,

PubMed: 28357710 ( click the link to review the publication )
Oncol Lett, 2017, 14(3):3463-3472

PubMed: 28927101 ( click the link to review the publication )

Blood, 2016, 128(25):2988-2999

PubMed: 27769957 ( click the link to review the publication )

J Am Heart Assoc, 2016, 5(8)

PubMed: 27473037 ( click the link to review the publication )

Am J Physiol Gastrointest Liver Physiol, 2016, 310(8):G539-49

PubMed: 26893158 ( click the link to review the publication )

Invest Ophthalmol Vis Sci, 2016, 57(14):6461-6473

PubMed: 27893888 ( click the link to review the publication )

Int Immunopharmacol, 2016, 35:155-162

PubMed: 27049289 ( click the link to review the publication )

Sci Rep, 2016, 6:28655

PubMed: 27353957 ( click the link to review the publication )

J Exp Med, 2015, 212(4):525-38

PubMed: 25824820 ( click the link to review the publication )

Mol Syst Biol, 2015, 11(3):797

PubMed: 25814555 ( click the link to review the publication )

Matrix Biol, 2015, 48:66-77

PubMed: 25989506 ( click the link to review the publication )

EBioMedicine, 2015, 2(12):1944-56

PubMed: 26844273 ( click the link to review the publication )

J Med Chem, 2015, 58(1):466-79

PubMed: 25478866 ( click the link to review the publication )

J Med Chem, 2015,

PubMed: ( click the link to review the publication )

Cell Death Dis, 2015, 6:e1781

PubMed: 26068789 ( click the link to review the publication )

Eur J Immunol, 2015,

PubMed: 25707450 ( click the link to review the publication )

Sci Rep, 2015, 5:15911

PubMed: 26568478 ( click the link to review the publication )

Stem Cell Reports, 2015, 4(3):489-502

PubMed: 25684228 ( click the link to review the publication )

Mol Cancer, 2014, 13:40

PubMed: 24571667 ( click the link to review the publication )

Stem Cell Reports, 2014, 3(1):34-43

PubMed: 25068120 ( click the link to review the publication )

Exp Gerontol, 2014, 52:55-69

PubMed: 24486130 ( click the link to review the publication )

PLoS One, 2014, 9(7):e103578

PubMed: 25073020 ( click the link to review the publication )

Julius Maximilians Universit, 2014, Kumari G

PubMed: ( click the link to review the publication )

Genes Cancer, 2014, 5(9-10):353-64

PubMed: 25352952 ( click the link to review the publication )

Int J Cancer, 2013, 134(3):575-86

PubMed: 23901045 ( click the link to review the publication )
Am J Physiol Lung Cell Mol Physiol, 2013, 305(10):L747-55

PubMed: 24039256 ( click the link to review the publication )

J Biol Chem, 2013, 288(23):16882-94

PubMed: 23629661 ( click the link to review the publication )

Biochem J, 2013, 449(2):497-506

PubMed: 23116132 ( click the link to review the publication )

Eur J Pharmacol, 2013, 701(1-3):96-105

PubMed: 23348708 ( click the link to review the publication )

PLoS One, 2013, 8(1):e54181

PubMed: 23349819 ( click the link to review the publication )

Physiol Rep, 2013, 1(5):e00078

PubMed: 24303162 ( click the link to review the publication )

University of Toronto , 2013, Department of Immunology

PubMed: ( click the link to review the publication )

Cell Host Microbe, 2013, 13(1):67-76

PubMed: 23332156 ( click the link to review the publication )

Blood, 2012, 119(26):6255-8

PubMed: 22555972 ( click the link to review the publication )

Cancer Lett, 2012, 324(1):98-108

PubMed: 22579651 ( click the link to review the publication )

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description

Features

The first p38 MAPK inhibitor to be tested in a phase III clinical trial.

Targets

JNK2 ^[1] ()	c-RAF ^[1] ()	Fyn ^[1] ()	p38α ^[1] (Cell-free assay)	p38α ^[7] ()
			0.1 nM(Kd)	38 nM

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. ^[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]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HOP-92	NUe1So9wT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUexeZlwUUN3ME2yOE4{QDN6IN88US=>	NGrNfHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
NCI-H2228	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MljVTWM2OD1{Mz62OlY5KM7:TR?=	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
CAPAN-1	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NHP0SXhKSzVyPUKyMlE5QDRizszN	NXTUWZV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
SK-MEL-1	NYrmVFVkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NW\KbZlmUUN3ME2yNE4{Pjh\|IN88US=>	NIHRVmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
DB	NWDqb4Q3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M37xb2lEPTB;MUiuO\|kzOyEQvF2=	NWDFUFhuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
AN3-CA	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Ml65TWM2OD1zOD6xJO69VQ>?	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
EW-13	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NH\EWlJKSzVyPUG3Mlk2OTZizszN	NHHQXYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
LC-2-ad	M13iUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NH25SY1KSzVyPUG3MlQ{PjZizszN	MmXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
ES8	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3vGUWlEPTB;MUeuNVY4KM7:TR?=	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
NCI-H1581	NEPqPY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVXnXFZoUUN3ME2xO{4xPDR5IN88US=>	M2LNdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
HMV-II	NE[4cW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NV7zXWp1UUN3ME2xOE4zOzB7IN88US=>	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
BEN	M1ThTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFr0PIFKSzVyPUGzMlEzPjRizszN	NXuzdFFnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
NBsusSR	MkPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkfITWM2OD1zMD64NlM2KM7:TR?=	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
MS-1	NYTZUZhwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NWTjTok6UUN3ME2xNE45OjN3IN88US=>	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
BFTC-905	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXzJR\|UxRTFyLkGyN\|Mh\|ryP	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
NCI-SNU-1	MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MoDrTWM2OD17LkC2O\|M6KM7:TR?=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
MPP-89	NHK3[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVvFSZB3UUN3ME24MlQ3OjVzIN88US=>	NV24VnN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
T-24	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1rz[WlEPTB;OD60NFY4OyEQvF2=	NEHIWms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
KP-N-YN	MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmfTTWM2OD16LkKwNVkh\|ryP	NF\5[os9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
IST-MES1	NIL2NJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYjJR\|UxRTdwOUW2N\|ch\|ryP	M{jhZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
NCI-H358	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXf4O4lsUUN3ME23MlU{QCEQvF2=	Mlz3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
GOTO	NIjhS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NHO4cmFKSzVyPU[uN\|kyPjFizszN	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
DU-145	MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1zXPWlEPTB;Mz65N\|gyOSEQvF2=	Mn3yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
EoL-1-cell	M3v1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXG2To94UUN3ME2wMlM1PzZ\|IN88US=>	NIDVR\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
KYSE-270	M2LVZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MUjJR\|UxRTJ2LkW1O\|Mh\|ryP	NXLh[oFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
HCC1806	NFTnWnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEO3[\|hKSzVyPUK0Mlc4QTlizszN	MkPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
HuO-3N1	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MVHJR\|UxRTJ3LkixPFUh\|ryP	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
HOS	MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MoewTWM2OD1{NT65NlkzKM7:TR?=	NX;zZWR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
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BL21(DE3)	MYLGeY5kfGmxbjDhd5NigQ>?		M3v4c2lvcGmkaYTpc44hd2ZicEO4ZYxxcGFiYXP0bZZmKG[xcn2g[ZhxemW\|c3XkJIlvKEW\|Y3jldolkcGmjIHPvcIkhSkx{MTjESVMqKGOnbHzzJIJ6KEiWUl[gZZN{[XluIFnDOVAhRSByLkK1JO69VS5?	NXvnUIJjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5Nlg5PThpPkG5PVI5QDV6PD;hQi=>
whole blood cells	M3fpXWFvfGmrbn\sZY1u[XSxcomgZZN{[Xl?	NHvCVHQ1KGi{cx?=	MlHKRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBpfW2jbjD3bI9t\SCkbH;v[EBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJHRPTmGucHjhJJBzd2S3Y4Tpc44h[W[2ZYKgOEBpenNiYomgeIlu\S2{ZYPvcJZm\CCobIXvdoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLk[g{txONg>?	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd2OUK4Nkc,OjJ5NEmyPFI9N2F-
A673	MlnZdWhVWyCjc4PhfS=>		MnvwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	MljJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
DAOY	MVrxTHRUKGG\|c3H5		M2DR[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy\|	MlfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
RD	MVHxTHRUKGG\|c3H5		NGHWTWhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN?	NVz5cFI3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	Mo\HdWhVWyCjc4PhfS=>		MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	NV3CcIRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R)	M3TWTpFJXFNiYYPzZZk>		M3XROZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	NUfob3kyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	MnrjdWhVWyCjc4PhfS=>		NFK0dY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	NXvoWJBzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	MnL6dWhVWyCjc4PhfS=>		NV2ye4JjeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-p38 / p38 ; PubMed: 23349819 PLoS One The inhibitory effect of phosphorylated p38 in KB, KBV200 (B) and in MCF-7, MCF-7/ADR (C) treated with BIRB796 at various concentrations after 24 h. mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 ; PubMed: 26844273 EBioMedicine CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot. p-p38 / γ-H2AX ; PubMed: 27082306 Cancer Biol Ther The expression of p-P38 was tested via protein gel blot after the cells were treated with BIRB796.	23349819 26844273 27082306

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

Protocol

Animal Research: ^[2]	- Collapse Animal Models: Collagen-induced arthritis in female Balb/c mice Dosages: 1 mg/kg (intravenous) or 10 mg/kg (oral) Administration: Intravenous injection or by oral (Only for Reference)

References

- Collapse

Solubility (25°C)

In vitro	DMSO	100 mg/mL (189.51 mM)
	Ethanol	100 mg/mL (189.51 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+40%PEG300+5%Tween80 +50%H2O For best results, use promptly after mixing.	5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Doramapimod (BIRB 796) SDF

Molecular Weight	527.66
Formula	C₃₁H₃₇N₅O₃
CAS No.	285983-48-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

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):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

Pan p38 MAPK Inhibitor

SB202190 (FHPI) : Pan-p38α/β inhibitor, IC50=50 nM/100 nM.
Most Potent p38 MAPK Inhibitor

Skepinone-L ^New : p38α-MAPK, IC50=5 nM.
p38 MAPK Inhibitor in Clinical Trial

PH-797804 : Phase II for Chronic Obstructive Pulmonary Disease (COPD).
Newest p38 MAPK Inhibitor

Skepinone-L ^New : Selective p38α-MAPK inhibitor with IC50 of 5 nM.

Related p38 MAPK Products

Pexmetinib (ARRY-614) ^New

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
SB239063 ^New

SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
Ravoxertinib (GDC-0994) ^New

Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
SB203580

SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

Features:First reported p38 inhibitor.
SB202190 (FHPI)

SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Ralimetinib dimesylate

Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
Losmapimod (GW856553X)

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
PH-797804

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
VX-702

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

Features:Highly selective, orally active inhibitor of p38 MAPK.
TAK-715

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

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Doramapimod (BIRB 796)