(+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells.(+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested.
|Cell lines||MC 11060 cells|
|Preparation method||Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism).|
|Incubation time||48 hours|
|Animal models||Mice bearing NMC 797 xenografts|
|Formulation||5% DMSO in 5% dextrose|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1.
Kumar K, et al. Sci Rep. 2015 Mar 25;5:9489. PMID: 25807524.
Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma.
Lee DH, et al. Int J Cancer. 2015 May 1;136(9):2055-64. PMID: 25307878.
|Related Epigenetic Reader Domain Products|
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.
GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains with a Kd of 89 nM.
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively.
ARV-771 is a small-molecule pan-BET degrader with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
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