9 Results for "

co-activator peptide

" in MedChemExpress (MCE) Product Catalog:
Products (9)

9 Results for "co-activator peptide" in MCE Product Catalog:

Cat. No.: HY-N10508
CAS No.: 71204-89-2
Calcitroic acid is a water-soluble terminal vitamin D metabolite and also a ligand for vitamin D receptor (VDR). Calcitroic acid binds to the ligand-binding domain of VDR, forms a retinoic X receptor complex, recruits the coactivator peptide MED1, mediates partial VDR-dependent transcription, inhibits Calcitriol (HY-10002)-induced VDR activation, and reduces the transcription level of CYP24A1 in the presence of 1α,25-dihydroxyvitamin D3. Calcitroic acid exerts selective activating effects on VDR, upregulates the expression of CYP24A1 and CYP3A4, decreases the transcription levels of iNOS and IL-1β, reduces the secretion of nitric oxide and IL-1β, and possesses metabolic stability due to its resistance to phase I oxidation and hepatic glucuronidation. Calcitroic acid can be used in research related to colon cancer, inflammatory bowel disease and rickets .
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Cat. No.: HY-33821
CAS No.: 171049-41-5
Target:  

LXR

Research Areas:  

Others

LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators .
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Cat. No.: HY-P11443
CAS No.: 245122-99-0
Target:  

Androgen Receptor

Research Areas:  

Cancer

SRC2-2 peptide is a a coactivator-derived mimic targeting androgen receptor (AR) ligand. SRC2-2 peptide is promising for research of prostate cancer .
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Cat. No.: HY-P5458
CAS No.: 394658-24-3
Research Areas:  

Others

SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
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Cat. No.: HY-P2515
CAS No.: 359821-54-8
Research Areas:  

Others

Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a TIF-2 coactivator peptide composed of 14 amino acids and covers the residue range 740-753 of TIF-2 protein .
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Cat. No.: HY-P10843
Target:  

Estrogen Receptor/ERR

Research Areas:  

Cancer

R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
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Cat. No.: HY-122222
CAS No.: 393794-32-6
Target:  

PPAR

Research Areas:  

Others

MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC50 being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC50 values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .
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Cat. No.: HY-183279
Target:  

FXR AMPK

Research Areas:  

Metabolic Disease

FXR antagonist 4 (Compound 4l) is an orally active, selective FXR antagonist with an IC50 of 0.70 μM. FXR antagonist 4 binds to FXR, differentially regulates bile acid and lipid transporter genes, and exerts no effect on gluconeogenesis-related genes. FXR modulator 1 activates the AMPK signaling pathway to inhibit fatty acid synthesis. FXR modulator 1 alleviates hepatic steatosis, ballooning degeneration and fibrosis, and improves dyslipidemia. FXR modulator 1 can be used for research on metabolic dysfunction-associated steatohepatitis .
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Cat. No.: HY-N10508S
CAS No.: 1637678-42-2
Calcitroic acid-13C is the 13C-labeled Calcitroic acid (HY-N10508). Calcitroic acid is a water-soluble terminal vitamin D metabolite and also a ligand for vitamin D receptor (VDR). Calcitroic acid binds to the ligand-binding domain of VDR, forms a retinoic X receptor complex, recruits the coactivator peptide MED1, mediates partial VDR-dependent transcription, inhibits Calcitriol (HY-10002)-induced VDR activation, and reduces the transcription level of CYP24A1 in the presence of 1α,25-dihydroxyvitamin D3. Calcitroic acid exerts selective activating effects on VDR, upregulates the expression of CYP24A1 and CYP3A4, decreases the transcription levels of iNOS and IL-1β, reduces the secretion of nitric oxide and IL-1β, and possesses metabolic stability due to its resistance to phase I oxidation and hepatic glucuronidation. Calcitroic acid can be used in research related to colon cancer, inflammatory bowel disease and rickets .
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