1. Epigenetics
  2. Epigenetic Reader Domain
  3. RVX-297

RVX-297 

Cat. No.: HY-114504
Handling Instructions

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.

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RVX-297 Chemical Structure

RVX-297 Chemical Structure

CAS No. : 1044871-04-6

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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].

IC50 & Target[2]

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.
Molecular Weight

423.50

Formula

C₂₄H₂₉N₃O₄

CAS No.

1044871-04-6

SMILES

O=C1NC(C2=CC(C)=C(OCCN3CCCC3)C(C)=C2)=NC4=C1C(OC)=CC(OC)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

RVX-297RVX297RVX 297Epigenetic Reader DomainselectivityinflammatoryimmunecellacuteautoimmunitymediatorproinflammatoryarthritisInhibitorinhibitorinhibit

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