1229096-88-1
Chemical Structure
GSK9027
- CAS No.: 1229096-88-1
- Formula:C27H19F4N3O2S
- Molecular Weight:525.52
IUPAC Name: N-(4-(1-(4-fluorophenyl)-1H-indazol-5-yl)-3-(trifluoromethyl)phenyl)-1-phenylmethanesulfonamide
InChIKey: DXBJGDVBQPEMOB-UHFFFAOYSA-N
SMILES: O=S(CC1=CC=CC=C1)(NC2=CC=C(C3=CC4=C(N(C5=CC=C(F)C=C5)N=C4)C=C3)C(C(F)(F)F)=C2)=O
Biological Activity: GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GSK9027 | 98.59% | GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone. | ||||||||||||||||||||
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OSU-03012 (Standard) | ≥98% | OSU-03012 (Standard) is the analytical standard of OSU-03012 (HY-10547). This product is intended for research and analytical applications. OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM. | ||||||||||||||||||||
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BTT-3033 | 96.57% | BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease. | ||||||||||||||||||||
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SR-3737 | SR-3737 is a JNK3 and p38 inhibitor (IC50: 12 and 3 nM). | |||||||||||||||||||||
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Setin-1 | Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a. | |||||||||||||||||||||
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OSU-03013 | OSU-03013 is a Celecoxib (HY-14398) analog. OSU-03013 can promote apoptosis, up-regulate E-cadherin, and down-regulate β-catenin, c-myc, Wnt1, and N-cadherin. OSU-03013 reduces cell migration and invasion. OSU-03013 regulates both Wnt and mTOR expression to inhibit colon cancer (CC) cell proliferation. OSU-03013 can be used for CC cancer research. | |||||||||||||||||||||
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COX-2/sEH-IN-1 | COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks. | |||||||||||||||||||||
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FASN-IN-6 | FASN-IN-6 (compound 44) is a potent fatty acid biosynthesis (FAB) inhibitor. FASN-IN-6 is an antibacterial agent with MICs of 1 μg/mL and 4 μg/mL for S. aureus ATCC 25923 and E. faecalis ATCC 29212, respectively. | |||||||||||||||||||||
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COX-2-IN-55 | 99.20% | COX-2-IN-55 (compound 1) is an orally active, Celecoxib (HY-14398)-based analog with broad-spectrum anticancer activity and weak COX-2 inhibition. COX-2-IN-55 specifically inhibits SERCA2, increases caspase-3 cleavage and DR5 levels, thereby activating GRP78 and inhibiting the development of triple-negative breast cancer (TNBC). COX-2-IN-55 can also downregulate the levels of angiogenic markers VEGF-α and IL-8, inhibiting the formation of microvessels. | ||||||||||||||||||||
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OSU-02067 | OSU-02067 is a selective 3-phosphoinositide-dependent protein kinase-1 (PDK-1) inhibitor (IC50=9 μM). OSU-02067 is promising for research of solid tumors (e.g., prostate, breast, colorectal cancers). | |||||||||||||||||||||
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TLX activator-1 | TLX activator-1 is a highly selective TLX activator with an EC50 of 0.010 μM. TLX activator-1 regulates gene expression, upregulates genes related to ATP production and lysosomal function, and inhibits genes associated with inflammatory signaling pathways and Apoptotic signaling pathways. TLX activator-1 exhibits anti-neurodegenerative activity. TLX activator-1 can be used for the research of neurodegenerative diseases. | |||||||||||||||||||||
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References
- [1]. Rider CF, et al. Cytokine-Induced Loss of Glucocorticoid Function: Effect of Kinase Inhibitors, Long-Acting β2-Adrenoceptor Agonist and Glucocorticoid Receptor Ligands. PLoS ONE. 2015; 10(1): e0116773.
- [2]. Rider, C. F., et al. TNF±-Induced Glucocorticoid Resistance: Inhibition Of Inflammatory Signalling And The Effect On Full And Partial GR Agonists. 2012