GSK 4112 (Synonyms: SR6452) |
| رقم الكتالوجGC10715 |
GSK 4112 (SR6452) عبارة عن ناهض Rev-erbα بقيمة EC50 تبلغ 0.4 ميكرومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1216744-19-2
Sample solution is provided at 25 µL, 10mM.
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IC50: 2.3 μM
GSK4112 is a synthetic antagonist of the Nuclear Heme Receptor REV-ERB.
Rev-erbα and Rev-erbβ are heme sensors and atypical members of the nuclear receptor superfamily. As a member of the nuclear receptor superfamily, REV-ERBR functions as a receptor for the porphoryin heme. REV-ERBR can suppress the transcription of its target genes in a heme-dependent manner.
In vitro: Previous study showed that GSK4112 addition to either the REV-ERBR or REV-ERBβ assay led to enhanced repression. Cells were treated the with GSK4112 and similar pattern in GAL4 chimeric receptor assay was observed. In addition, GSK4112 suppressed reporter gene expression. GSK4112 also suppressed transcription driven by the Bmal1 promoter dose-dependently. GSK4112 activity was found to be associated with REV-ERBR [1].
In vivo: GSK4112 was found to display poor pharmacokinetic properties (rat liver microsomal Cint > 1.0 mL/min/mg protein; lack of oral bioavailability (F < 1% in mice)), which likely limited its use to biochemical and cell-based assays. As a result, GSK4112 was unlikely to be suitable for in vivo studies [1].
Clinical trial: N/A
Reference:
[1] Daniel Grant,Lei Yin,Jon L. Collins et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear Heme receptor Rev-erbα. ACS CHEMICAL BIOLOGY5(10):925-32.
| Cas No. | 1216744-19-2 | SDF | |
| المرادفات | SR6452 | ||
| Formula | C18H21ClN2O4S | M.Wt | 396.89 |
| الذوبان | ≥ 11.9mg/mL in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5196 mL | 12.5979 mL | 25.1959 mL |
| 5 mM | 0.5039 mL | 2.5196 mL | 5.0392 mL |
| 10 mM | 0.252 mL | 1.2598 mL | 2.5196 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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 40 reference(s) in Google Scholar.)
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