1044871-04-6
1044871-04-6 structure
- Name: RVX-297
- Chemical Name: RVX297
- CAS Number: 1044871-04-6
- Molecular Formula:
- Molecular Weight:
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2018-07-18 11:48:42
- Modify Date: 2024-01-09 20:47:56
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RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2].
| Name | RVX297 |
|---|
| Description | RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2]. |
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| Related Catalog | |
| Target |
BRD2 (BD1):3.76 μM (IC50) BRD2 (BD2):0.08 μM (IC50) BRD3 (BD1):2.34 μM (IC50) BRD3 (BD2):0.05 μM (IC50) BRD4 (BD1):1.16 μM (IC50) BRD4 (BD2):0.02 μM (IC50) BRDT (BD1):2.69 μM (IC50) |
| In Vitro | RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts[1]. RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs[1]. RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression[1]. RT-PCR[1] Cell Line: Synovial fibroblasts Concentration: 1-30 μM Incubation Time: 24 hours Result: Downregulated IL-6 and VCAM-1 gene expression in synovial fibroblasts. |
| In Vivo | RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model[1]. RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model[1]. RVX-297 suppresses cytokine production in LPS-treated mice[1]. Animal Model: Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)[1] Dosage: 25, 50, and 75 mg/kg Administration: P.o.; per day for 6 days Result: Prevented swelling and inflammation of the ankle and knee joints. |
| References |
| No Any Chemical & Physical Properties |