| Bioactivity | CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM[1]. | ||||||||||||
| Invitro | CCG-63802 (5 μM) inhibits regulators of G-protein signaling (RGS) proteins in the presence of BK (bradykinin) and 8-Br-cGMP (membrane-permeable analogue of cGMP), HEK-293 cells start to depolarize again[2]. | ||||||||||||
| In Vivo | CCG-63802 (0.05 mg/kg; intratracheal administration; once per week; 90 days) reduces RGS4 protein expression, leading to partially abrogate the attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling[3]. Animal Model: | ||||||||||||
| Name | CCG-63802 | ||||||||||||
| CAS | 620112-78-9 | ||||||||||||
| Formula | C26H18N4O2S | ||||||||||||
| Molar Mass | 450.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Levi L Blazer, et al. Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol. 2010 Sep;78(3):524-33. [2]. Marina Dobrivojević, et al. Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1260-8. [3]. Xia Meng, et al. PPARγ Agonist PGZ Attenuates OVA-Induced Airway Inflammation and Airway Remodeling via RGS4 Signaling in Mouse Model. Inflammation. 2018 Dec;41(6):2079-2089. |
CCG-63802
CAS: 620112-78-9 F: C26H18N4O2S W: 450.51
CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the
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