Referencia número: HY-16652

Apabetalone

(Synonyms: RVX-208; RVX000222)

9 Cited Publications

Revisión del cliente

Based on 9 publication(s) in Google Scholar

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC₅₀s are 87 μM and 0.51 μM for BD1 and BD2, respectively.

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Pureza: 99.34%
No. CAS: 1044870-39-4
Fòrmula: C₂₀H₂₂N₂O₅
Peso molecular:370.40

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Apabetalone Chemical Structure

No. CAS: 1044870-39-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (9)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 510±41 nM (BD2), 87±10 μM (BD1)^[1]

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

Ver todos los productos específicos de isoformas HIV :

Cellular Effect

Cell Line	Type	Value	Description	References
697	EC₅₀	>5 μM Compound: 3; RVX-208	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
A2780	IC₅₀	122.6 μM Compound: RVX-208	Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
A-375	IC₅₀	240.9 μM Compound: RVX-208	Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A549	IC₅₀	53.1 μM Compound: RVX-208	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
CCRF-CEM	EC₅₀	>5 μM Compound: RVX-028	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
DLD-1	IC₅₀	>10 μM Compound: RVX-208	Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
ES-2	IC₅₀	8.01 μM Compound: RVX-208	Antiproliferative activity against human ES2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human ES2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
HCT-116	IC₅₀	12.83 μM Compound: RVX-208	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
HepG2	IC₅₀	103 μM Compound: RVX-208	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
HL-60	IC₅₀	>20 μM Compound: 2; RVX-208	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
HT-29	IC₅₀	235.8 μM Compound: RVX-208	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
K562	EC₅₀	>5 μM Compound: RVX-028	Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
L02	IC₅₀	>100 μM Compound: RVX-208	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay	[PMID: 30926312]
LOUCY	EC₅₀	>5 μM Compound: 3; RVX-208	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
MCF7	IC₅₀	>300 μM Compound: RVX-208	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
MCF7	IC₅₀	140.1 μM Compound: 2a; RVX-208	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 29172540]
MDA-MB-231	IC₅₀	155.4 μM Compound: 2a; RVX-208	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29172540]
MOLM-14	EC₅₀	6.7 μM Compound: RVX-028	Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
MV4-11	IC₅₀	>20 μM Compound: 2; RVX-208	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
MV4-11	IC₅₀	4.48 μM Compound: 1; RVX-208	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 28765013]
NALM-6	EC₅₀	>5 μM Compound: 3; RVX-208	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
NB-4	EC₅₀	>5 μM Compound: RVX-028	Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
NRK-49F	IC₅₀	42 μM Compound: RVX-208	Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
OCI-AML2	IC₅₀	8.31 μM Compound: 1; RVX-208	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	[PMID: 28765013]
OCI-AML-3	IC₅₀	7.17 μM Compound: 1; RVX-208	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 28765013]
OVCAR-3	IC₅₀	16.89 μM Compound: RVX-208	Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
SK-OV-3	IC₅₀	7.05 μM Compound: RVX-208	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
SW-620	IC₅₀	>10 μM Compound: RVX-208	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
SW626	IC₅₀	8.45 μM Compound: RVX-208	Antiproliferative activity against human SW626 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human SW626 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
U-937	IC₅₀	>20 μM Compound: 2; RVX-208	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]

In Vitro

Apabetalone (RVX-208) competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructs of the four BET proteins, with IC₅₀s between 0.5 and 1.8 μM. Apabetalone increases the production of ApoA-I in hepatocytes in vitro, which results in increased high density lipoprotein cholesterol (HDL-C). Apabetalone selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. Apabetalone increases Apolipoprotein A-I (ApoA-I) production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Apabetalone increases ApoA-I expression in liver cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In the atherosclerosis prophylactic treatment study design, mice are fed a Western diet concurrent with the treatment with 150 mg/kg/dose b.i.d. for 12 weeks. Mice are sacrificed at 12 weeks after treatment. There is a progressive increase in body weight in both the vehicle treated as well as the Apabetalone (RVX-208) treated groups. However, there is only an increase of 4 g (from 24 g to 28 g) body weight after 12 weeks on Western diet in the Apabetalone treated group whereas this increase is found to be 9 g (25 g-34 g) in the vehicle treated group. The significant decrease in body weight gain in Apabetalone treated mice is not due to decreased feed consumption, suggesting a positive attribute of the molecule. Plasma lipid measurements are done at 6 weeks and 12 weeks of treatment with either the vehicle or Apabetalone. Compared to the vehicle control animals, Apabetalone treated mice show significant increase (~200%) in the levels of HDL-C at 6 weeks of treatment, which is sustained until end of the study (12 weeks)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1044870-39-4
Appearance Solid
Peso molecular 370.40
Fòrmula C₂₀H₂₂N₂O₅
Color White to yellow
SMILES

COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1
Synonyms

RVX-208; RVX000222
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (9)

All WBCell Imaging/StainingMicrobiological AssayCell Migration/Invasion AssayRT-PCR

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Journal Impact Factor

Cell

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection. [Abstract]

2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809

Apabetalone purchased from MedChemExpress. Usage Cited in: Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]

Bromodomain and extraterminal protein inhibitors specific (RVX-2157) or selective (Apabetalone (25 μM)) for bromodomain 2 decrease ACE2 expression after 3 days.

Apabetalone purchased from MedChemExpress. Usage Cited in: Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]

Apabetalone (30 μM) or JQ-1 3-day pre-treatment reduces SARS-CoV-2 titer in hPSC-CM 3 days after infection.

Apabetalone purchased from MedChemExpress. Usage Cited in: Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]

Apabetalone (0.1-30 μM) 3-day pre-treatment to reduce SARS-CoV-2 infection. E-gene expression in 2D cultures 3 days after infection.
Cell Rep

BET-induced metabolic reprogramming fuels inflammation at the vascular-fat interface in mice and patients with cardiometabolic disease. [Abstract]

2026 Jun 23;45(6):117365. PMID: 42228564
Elife

Cohesin mutations are synthetic lethal with stimulation of WNT signaling. [Abstract]

2020 Dec 7;9:e61405. PMID: 33284104
Antioxid Redox Signal

The BET Protein Inhibitor Apabetalone Rescues Diabetes-Induced Impairment of Angiogenic Response by Epigenetic Regulation of Thrombospondin-1. [Abstract]

2022 Apr;36(10-12):667-684. PMID: 34913726

Apabetalone purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2022 Apr;36(10-12):667-684. [Abstract]

Representative images and relative quantification of Matrigel-based tube formation assay in the different experimental groups. The yellow arrow indicates loop formation in NG-treated cells. LO, loop; n = 6/group. Apabetalone (APA) (25 μM; 48 h) effectively rescued high glucose-induced impairment of angiogenic responses in HAECs.

Apabetalone purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2022 Apr;36(10-12):667-684. [Abstract]

Scratch assay and relative quantification showing migration of HG-treated HAECs, in the presence of APA or vehicle. n = 6/group. Apabetalone (APA, 25 μM; 48 h) reversed the inhibitory effect of high glucose on the migration ability of HAECs.
J Mol Cell Cardiol

Inhibition of BRD4 attenuates transverse aortic constriction- and TGF-β-induced endothelial-mesenchymal transition and cardiac fibrosis. [Abstract]

2019 Feb:127:83-96. PMID: 30529267
Biochim Biophys Acta

BET bromodomain is a novel regulator of TAZ and its activity. [Abstract]

2016 Dec;1859(12):1527-1537. PMID: 27717711

Apabetalone purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537. [Abstract]

RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.
Dis Model Mech

Lamin variants cause cardiac arrhythmogenicity in Drosophila. [Abstract]

2025 Jul 1;18(7):dmm052424. PMID: 40605555
Addict Biol

The Selective Bromodomain and Extra-Terminal Domain (BET) Inhibitor RVX-208 Reduces Cocaine-Seeking Behaviour and Alters Proteomic Pathways in the Nucleus Accumbens. [Abstract]

2026 Jan;31(1):e70121. PMID: 41507765
Patent

US20180263995A1.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 33 mg/mL (89.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6998 mL

13.4989 mL

26.9978 mL

5 mM

0.5400 mL

2.6998 mL

5.3996 mL

10 mM

0.2700 mL

1.3499 mL

2.6998 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline