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General description
A cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain) family members BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity (Kd = 61.3, 50.5, and 55.2 nM, respectively, by ITC) and effectively competes against tetra-acetylated H4 peptide (Millipore cat. no. 12-379) for BRD2/3/4 binding (IC50 = 32.5, 42,4, and 36.1 nM, respectively, in competitive equilibrium binding assays), while exhibiting little affinity toward 5 other bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140) or a panel of 38 cellular enzymes, GPCRs, transporters, and ion channels. Shown to differentially modulate LPS-induced gene expression, notably suppressing LPS-induced upregulation of genes involved in inflammatory response, in murine BMDMs (bone marrow-derived macrophages) in vitro (30 min 1 µM pretreatment) and effectively prevent LPS-, heat-killed Salmonella typhimurium-, and CLP- (caecal ligation and puncture) induced death in mice in vivo (30 mg/kg i.v.). Cellular Brd2/3/4 knockdown using siRNA results in mostly the same effect as I-BET treatment in modulating LPS gene induction profile in murine BMDMs, but not without exceptions, indicating that not all BET-dependent transcription regulations are mediated via its binding to acetylated histones.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
tandem bromodomains of BET
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.
Other Notes
Nicodeme, E., et al. 2010. Nature468, 1119.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,desiccated (hygroscopic),protect from light |
| storage temp. | −70°C |
| SMILES string | Clc1ccc(cc1)C2=N[C@H](c3[n](c(nn3)C)c4c2cc(cc4)OC)CC(=O)NCC |
| InChI | 1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1 |
| InChI key | AAAQFGUYHFJNHI-SFHVURJKSA-N |
| 长度(mm) | |
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