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Immunoway/(+)-JQ1/10mg 50mg 100mg/MC0256
市场价：
¥3600.00
美元价：
1800.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
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(+)-JQ1
- Catalog No.：MC0256
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1268524-70-4
- MolecularFormula：
- C23H25ClN4O2S
- Purity：
- HPLC Purity>99%,ee purity>99%
- Target：
- Epigenetic Reader Domain
- IC50：
- IC50: 77/33 nM (BRD4(1/2))[1]
- In Vitro：
- (+)-JQ1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)[1]. (+)-JQ1 is a potent thienodiazepine inhibitor (Kd=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ1 demonstrates potent inhibition of H4Kac4 binding with a IC50 value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1)[2].
- In Vivo：
- Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL)[1].
- Fields：
- (+)-JQ1 is a BET bromodomain inhibitor, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. IC50: 77/33 nM (BRD4(1/2))[1]
- Specificity：
- Target:Epigenetic Reader Domain . Fields: (+)-JQ1 is a BET bromodomain inhibitor, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. IC50: 77/33 nM (BRD4(
- Source：
- Rabbit
- Dilution：
- IC50: 77/33 nM (BRD4(1/2))[1]
- Concentration：
- HPLC Purity>99%,ee purity>99%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- JQ-1，JQ 1，JQ1，+JQ 1，+JQ-1，+JQ1
- MolecularWeight(Da)：
- 456.99
- References：
- [1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.[2]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2
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