GSK046 (Synonyms: GSK046) |
| Katalog-Nr.GC60182 |
GSK046 (iBET-BD2) ist ein potenter, selektiver und oral aktiver BD2-BromodomÄnen-Inhibitor der BET-Proteine mit IC50-Werten von 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) und 214 nM (BRDT BD2), bzw.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2474876-09-8
Sample solution is provided at 25 µL, 10mM.
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GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively[1].
GSK046 (1000 nM; refresh every three days) reduces the recruitment of BET proteins to interferon (IFN) target genes following IFN-γ stimulation. GSK046 appears to more prominently affect the recruitment of BRD2 and BRD3 compared to BRD4[1].GSK046 (0.1-10 μM) displays a more selective phenotypic fingerprint, particularly inhibiting the production of key pro-inflammatory mediators including Th17 cytokines in the B and T cell co-culture system[1].GSK046 (0.01-10 μM; 72 hours) does not affect the proliferative activity of human primary CD4+ T cells but still inhibits the production of effector cytokines including IFNγ, IL-17A and IL-22[1].GSK046 (0.005-10 μM; 48 hours) impairs macrophage activation following PMA stimulation, without impacting cellular viability[1]. Cell Proliferation Assay[1] Cell Line: Human primary CD4+ T cell
GSK046 (40 mg/kg/QD; s.c. for 14 days) has immunomodulatory activity[1].GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg)[1].GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1]. Animal Model: Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)[1]
[1]. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394.
| Cas No. | 2474876-09-8 | SDF | |
| Überlieferungen | GSK046 | ||
| Canonical SMILES | O=C(N[C@H]1CC[C@H](O)CC1)C2=CC(O[C@H](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2 | ||
| Formula | C23H27FN2O4 | M.Wt | 414.47 |
| Löslichkeit | DMSO : 83.33 mg/mL (201.05 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4127 mL | 12.0636 mL | 24.1272 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8254 mL |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4127 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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