(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway.way.
Nat Commun. 2023 Mar 14;14(1):1413.
BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism
(+)-JQ1 purchased from AbMole
JCI Insight. 2022 Sep 8;7(17):e151851.
Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
(+)-JQ1 purchased from AbMole
J Exp Med. 2022 Nov 7;219(11):e20212405.
Transit-amplifying cells control R-spondins in the mouse crypt to modulate intestinal stem cell proliferation
(+)-JQ1 purchased from AbMole
Cancer Cell. 2016 Aug 8;30(2):290-307.
Regulation of OGT by URI in Response to Glucose Confers c-MYC-Dependent Survival Mechanisms
(+)-JQ1 purchased from AbMole
Oncotarget. 2015 Nov 10;6(35):37410-25.
SMAC mimetic Debio 1143 synergizes with taxanes, topoisomerase inhibitors and bromodomain inhibitors to impede growth of lung adenocarcinoma cells
(+)-JQ1 purchased from AbMole
Cell Experiment | |
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Cell lines | MM.1S, RPMI-8226, KMS-20, L-363 Dox40 and AMO-1 cell lines |
Preparation method | Cell Viability Assays MM cell lines were seeded onto 384-well tissue culture treated plates at a density of 1,000 cells/well in a volume of 50 µL of media. After seeding cells were incubated for 1 hour and during the interim a stock plate of JQ1 was thawed at room temperature in a desiccated box. The addition of JQ1 to the assay plate was done with disposable 384-well pins (V&P Scientific, San Diego, CA) that delivered 100 nL of the drug diluted in DMSO to each well of the plate. After 72 hours of incubation cells were analyzed for cell viability by the addition of CellTiter Glo (Promega, Madison, WI) to the assay plates. After 30 min incubation at 37 oC the signal from the viable cells was analyzed on a Luminoskan luminometer (Labsystems Franklin, MA). |
Concentrations | 0~1µM |
Incubation time | 72 h |
Animal Experiment | |
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Animal models | SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells |
Formulation | JQ1 in 10% cyclodextrine (Sigma) |
Dosages | 50 mg/kg daily |
Administration | intra-peritoneally for 5 days/week, 2 weeks |
Molecular Weight | 456.99 |
Formula | C23H25ClN4O2S |
CAS Number | 1268524-70-4 |
Solubility (25°C) | DMSO 45 mg/mL Ethanol 45 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Matzuk MM, et al. Cell. Small-molecule inhibition of BRDT for male contraception.
[3] Delmore JE, et al. Cell. BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
[4] Filippakopoulos P, et al. Nature. Selective inhibition of BET bromodomains.
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