Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Molibresib [1260907-17-2]

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Referência HY-13032-5mg

Tamanho : 5mg

Marca : MedChemExpress

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Description

Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

IC₅₀ & Target

IC50: 32.5-42.5 nM (BET)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
697	EC₅₀	1.17 μM Compound: 2; GSK525762A	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]
HepG2	EC₅₀	700 nM Compound: 2, GSK525762A	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay	[PMID: 21568322]
HepG2	EC₅₀	700 nM Compound: 3, I-BET762, GSK525762A	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay	[PMID: 22924434]
HL-60	IC₅₀	0.12 μM Compound: I-BET762	Cytotoxicity against human HL60 cells by MTS assay Cytotoxicity against human HL60 cells by MTS assay	[PMID: 29657099]
K562	IC₅₀	>2000 nM Compound: 2, I-BET-762	Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
K562	IC₅₀	>2 μM Compound: 2, I-BET-762	Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
Kasumi 1	IC₅₀	0.21 μM Compound: 1; IBET762	Antiproliferative activity against human Kasumi-1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human Kasumi-1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30905542]
LNCaP	IC₅₀	356.5 nM Compound: 2; I-BET762	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 29758518]
LOUCY	EC₅₀	>5 μM Compound: 2; GSK525762A	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]
MM1.S	IC₅₀	0.23 μM Compound: 2; I-BET762	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 28586718]
MM1.S	IC₅₀	141 nM Compound: 1; I-BET762	Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MM1.S	IC₅₀	349.2 nM Compound: 2; I-BET762	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 29525435]
MOLM-13	IC₅₀	241 nM Compound: 2, I-BET-762	Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MOLM-13	IC₅₀	241 nM Compound: 4; I-BET762	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	0.8 μM Compound: 1; I-BET762	Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay	[PMID: 30268702]
MV4-11	IC₅₀	0.8 μM Compound: 1; IBET762	Cytotoxicity against human MV4-11 cells assessed as inhibition of cell viability Cytotoxicity against human MV4-11 cells assessed as inhibition of cell viability	[PMID: 30905542]
MV4-11	IC₅₀	1.23 μM Compound: I-BET-762	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
MV4-11	IC₅₀	102 nM Compound: I-BET762, GSK525762A	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 21964340]
MV4-11	IC₅₀	112 nM Compound: 1; I-BET762	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MV4-11	IC₅₀	93 nM Compound: 2, I-BET-762	Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MV4-11	IC₅₀	93 nM Compound: 4; I-BET762	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay	[PMID: 28463487]
NALM-6	EC₅₀	0.39 μM Compound: 2; GSK525762A	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]
PBMC	IC₅₀	0.2 μM Compound: I-BET762, GSK525762A	Anti-inflammatory activity against LPS-stimulated human PBMC assessed as IL-6 production Anti-inflammatory activity against LPS-stimulated human PBMC assessed as IL-6 production	[PMID: 21964340]
Raji	IC₅₀	0.19 μM Compound: I-BET762	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	[PMID: 24900758]
THP-1	IC₅₀	0.29 μM Compound: III; I-BET762; GSK-525762A	Antiproliferative activity against human THP1 cells Antiproliferative activity against human THP1 cells	[PMID: 28939121]

In Vitro

Molibresib (I-BET 762) shows the highest affinity interaction with BET. Molibresib binds to the tandem bromodomains of BET with high affinity (dissociation constant K_d of 50.5-61.3 nM). Molibresib displaces, with high efficacy (half-maximum inhibitory concentration IC₅₀ of 32.5-42.5 nM), a tetra-acetylated H4 peptide that had been pre-bound to tandem bromodomains of BET^[1]. Molibresib has high affinity for BD1/BD2 domain of BRD2/3/4 proteins. Molibresib treatment leads to a reduction in the recruitment of all three proteins to chromatin^[2]. Molibresib inhibits OPM-2 cell proliferation with IC₅₀ of 60.15 nM^[3].

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

Solvant et solubilité

In Vitro:

DMSO : 200 mg/mL (471.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1M HCl : 100 mg/mL (235.90 mM; ultrasonic and adjust pH to 1 with HCl)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3590 mL	11.7952 mL	23.5905 mL
5 mM	0.4718 mL	2.3590 mL	4.7181 mL
10 mM	0.2359 mL	1.1795 mL	2.3590 mL

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
Protocol 4

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.18 mM); Clear solution

Pureté et documentation

Purity: 99.94%

Fiche technique (283 KB) SDS (393 KB)

COA (253 KB) LCMS (95 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. [Content Brief]

[2]. Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. [Content Brief]

[3]. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705. [Content Brief]

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Marca : MedChemExpress

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