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JQ-1 carboxylic acid, a type of (+)-JQ-1 derivative, is a potent BET bromodomain inhibitor for downregulating PD-L1 expression on the surface of tumor cells. JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains.
| Cell Experiment | |
|---|---|
| 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). |
| Concentrations | ~500 nM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing NMC 797 xenografts |
| Formulation | 5% DMSO in 5% dextrose |
| Dosages | 50 mg/kg |
| Administration | intraperitoneal injection |
| Molecular Weight | 400.88 |
| Formula | C19H17ClN4O2S |
| CAS Number | 202592-23-2 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| dBRD9 dihydrochloride
dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. |
| BBC0403
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. |
| BAY-155
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. |
| FHT-1015
FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM. |
| ISOX-DUAL
ISOX-DUAL is a dual CBP/BRD4 inhibitor with IC50 values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively. |
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