JQ-1 free base · Synonyms: JQ1
-JQ-1, a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor.
For research use only. Not for human or veterinary use.
JQ-1 structure
CAS No.: 1268524-70-4
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 500 mg | USD 498.00 | BP-02472-500mg | In stock | Get quote |
| 1 g | USD 796.00 | BP-02472-1g | In stock | Get quote |
| 2 g | USD 1,274.00 | BP-02472-2g | In stock | Get quote |
| 3 g | USD 1,520.00 | BP-02472-3g | In stock | Get quote |
| 5 g | USD 2,040.00 | BP-02472-5g | In stock | Get quote |
| 10 g | USD 3,260.00 | BP-02472-10g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .
Biological activity
In Vitro (+)-JQ-1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ-1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ-1 (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.(+)-JQ-1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)[1]. De-repression of autophagy genes is observed almost immediately after (+)-JQ-1 addition[2]. (+)-JQ-1 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 (+)-JQ-1 demonstrates potent inhibition of H4Kac4 binding with a IC50 value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1). In Vivo Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. 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).
Identifiers
- SMILES
-
CC1=NN=C2[C@H](CC(=O)OC(C)(C)C)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1 - InChIKey
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DNVXATUJJDPFDM-KRWDZBQOSA-N
Specifications
- MW (average)
- 456.9880
- Formula
- C23H25ClN4O2S
- CAS No.
- 1268524-70-4
- Physical state
- Solid
- Color
- White to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 6 months;
Solubility
Soluble in DMSO
Documents
- CoA On request
- Handling Instructions