2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. REV-ERB
  4. GSK1362

GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS (HY-D1056)-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases.

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GSK1362

GSK1362 Chemical Structure

CAS No. : 2986733-57-5

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GSK1362 Related Antibodies

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Description

GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS (HY-D1056)-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases[1].

In Vitro

GSK1362 (24 h) increases transcription in a concentration-dependent manner in HEK293 cells cotransfected with HA-Rev-Erbα and Bmal1-Luc reporter, exerting an inverse agonist effect to relieve BMAL1 repression by endogenous REV-ERB ligands like heme[1].
GSK1362 (10 μM, 4 h) inhibits LPS (HY-D1056)-induced production of several inflammatory cytokines in alveolar macrophages collected at ZT8[1].
GSK1362 (10 μM, 16 h) inhibits the induction of Cxcl5 transcription in serum shock-synchronized mouse LA-4 cells[1].
GSK1362 (10 μM, 4 h) significantly increases REV-ERBα protein abundance in serum shock-synchronized human primary bronchial epithelial (NHBE) cells[1].
GSK1362 (10 μM, pretreated for 15 min) stabilizes REV-ERBα protein and counteracts IL-1β-induced REV-ERBα protein degradation in serum shock-synchronized NHBE cells[1].
GSK1362 (10 μM, 4 h) blocks IL-1β or TNF-α-induced ubiquitination of REV-ERBα in HEK293T cells transfected with HA-Rev-Erbα, His-Ub and SENP-1 plasmids[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK1362 Related Antibodies
Molecular Weight

396.87

Formula

C21H21ClN4O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=C(NCCOC)OC(C2=CC=C(N(CC3=CC=C(C=C3)Cl)C)C=C2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (251.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5197 mL 12.5986 mL 25.1972 mL
5 mM 0.5039 mL 2.5197 mL 5.0394 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5197 mL 12.5986 mL 25.1972 mL 62.9929 mL
5 mM 0.5039 mL 2.5197 mL 5.0394 mL 12.5986 mL
10 mM 0.2520 mL 1.2599 mL 2.5197 mL 6.2993 mL
15 mM 0.1680 mL 0.8399 mL 1.6798 mL 4.1995 mL
20 mM 0.1260 mL 0.6299 mL 1.2599 mL 3.1496 mL
25 mM 0.1008 mL 0.5039 mL 1.0079 mL 2.5197 mL
30 mM 0.0840 mL 0.4200 mL 0.8399 mL 2.0998 mL
40 mM 0.0630 mL 0.3150 mL 0.6299 mL 1.5748 mL
50 mM 0.0504 mL 0.2520 mL 0.5039 mL 1.2599 mL
60 mM 0.0420 mL 0.2100 mL 0.4200 mL 1.0499 mL
80 mM 0.0315 mL 0.1575 mL 0.3150 mL 0.7874 mL
100 mM 0.0252 mL 0.1260 mL 0.2520 mL 0.6299 mL
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GSK1362 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK13622986733-57-5GSK 1362GSK-1362REV-ERBinflammatory diseasesREV-ERBαNCoR1SMRT2RIP140Inhibitorinhibitorinhibit

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