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Doramapimod (BIRB-796)

  Cat. No.:  DC7836   Featured
Chemical Structure
285983-48-4
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Field of application
BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 285983-48-4
Chemical Name: 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea
Synonyms: BIRB 796; BIRB-796; BIRB796,
SMILES: O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3
Formula: C31H37N5O3
M.Wt: 527.66
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Doramapimod (BIRB 796) is a highly potent p38 MAPK inhibitor with an IC50 of 4 nM. It also inhibits B-Raf with an IC50 of 83 nM.
In Vivo: The mean xenograft weigh of Doramapimod (BIRB 796) plus Paclitaxel group (1.14±0.48 g) is lighter than control, Doramapimod or Paclitaxel group (1.84±0.61, 1.80±0.62 and 1.65±0.29 g) (P<0.05) in Athymic nude mice (BALB/c-nu/nu). The inhibition rate of Doramapimod, Paclitaxel and Doramapimod plus Paclitaxel is 1.93%, 9.93% and 38%. Importantly, the combination of Doramapimod and Paclitaxel produces a significant inhibition of tumor growth, compare with control, Paclitaxel or Doramapimod alone[4]. The Doramapimod (BIRB 796) treatment slightly reduces blood pressure (166±7 mm Hg at week 7; P<0.05), whereas SD rats are normotensive (123±3 mm Hg). Despite the reduction in blood pressure, untreated and Doramapimod-treated dTGRs have similar heart weight and cardiac hypertrophy indices (heart-to-tibia ratio), which are significantly higher compare with nontransgenic SD rats (310±6 versus 307±6 versus 206±5 mg/cm, respectively; P<0.05)[5].
In Vitro: Doramapimod (BIRB 796) is a highly potent inhibitor of p38α, a serine/threonine mitogen activated protein kinase (MAPK) that is usually associated with inflammation because of its role in T-cell proliferation and cytokine production[1]. Doramapimod (BIRB 796) is a picomolar inhibitor of human p38 MAP kinase[2]. HEK293 cells are incubated with different concentrations of Doramapimod (BIRB 796) for 30 min or 2 h prior to stimulation with sorbitol (an osmotic shock) and examined the activation of MAPKAP-K2 by measuring its activity. MAPKAP-K2 activation is inhibited in these cells in a time-dependent manner with an apparent IC50 of 30 nM after 30 min or 8 nM after 2 h of preincubation with Doramapimod[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7028 SB242235 SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.
DC9300 TA-02 TA-02 induces cardiomyocyte differentiation from human embryonic stem cells following mesoderm induction. Potently inhibits p38α, CK1δ and CK1ε (IC50 values are 20, 32 and 32 nM respectively).
DC7946 SKF-86002 SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).
DC1004 SB-203580 SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM and blocks PKB phosphorylation with IC50 of 3-5 μM.
DC7807 SB 239063 SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
DC2097 SB202190 SB 202190 is a pyridinyl imidazole that inhibits the p38 pathway.
DC5095 PD169316 PD169316 is a potent and selective p38 MAP kinase inhibitor
DC9681 Pamapimod（R-1503） Pamapimod（R-1503）is a novel p38 MAP kinase inhibitor.
DC8630 Ralimetinib 2MsOH(LY2228820) LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).
DC7836 Doramapimod (BIRB-796) BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.
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