Art. -Nr.: HY-101567

BMS-986158

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

BMS-986158 is a potent BET inhibitor with IC₅₀s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.

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Reinheit: 99.75%
CAS. Nr.: 1800340-40-2
Formel: C₃₀H₃₃N₅O₂
Molecular Weight:495.62

Speicherung:

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

BMS-986158 Chemical Structure

CAS. Nr.: 1800340-40-2

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BMS-986158 is a potent BET inhibitor with IC₅₀s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively^[1].

IC₅₀ & Target

IC50: 6.6 nM (BET, in NCI-H211 SCLC cells), 5 nM (in MDA-MB231 TNBC) cells)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human A549 cells Anticancer activity against human A549 cells	[PMID: 34543572]
DMS-114	IC₅₀	0.32 nM Compound: 18; BMS-986158	Anticancer activity against human DMS-114 cells Anticancer activity against human DMS-114 cells	[PMID: 34543572]
DMS-53	IC₅₀	0.29 nM Compound: 18; BMS-986158	Anticancer activity against human DMS-53 cells Anticancer activity against human DMS-53 cells	[PMID: 34543572]
HCC44	IC₅₀	2.7 nM Compound: 18; BMS-986158	Anticancer activity against human HCC44 cells Anticancer activity against human HCC44 cells	[PMID: 34543572]
HCC95	IC₅₀	8.1 nM Compound: 18; BMS-986158	Anticancer activity against human HCC95 cells Anticancer activity against human HCC95 cells	[PMID: 34543572]
MDA-MB-231	IC₅₀	4.97 nM Compound: 1; BMS-986158	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTS assay	[PMID: 36893627]
MOLM-13	IC₅₀	1.7 nM Compound: 18; BMS-986158	Anticancer activity against human MOLM-13 cells Anticancer activity against human MOLM-13 cells	[PMID: 34543572]
NCI-H1048	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1048 cells Anticancer activity against human NCI-H1048 cells	[PMID: 34543572]
NCI-H1355	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1355 cells Anticancer activity against human NCI-H1355 cells	[PMID: 34543572]
NCI-H146	IC₅₀	0.41 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H146 cells Anticancer activity against human NCI-H146 cells	[PMID: 34543572]
NCI-H1623	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1623 cells Anticancer activity against human NCI-H1623 cells	[PMID: 34543572]
NCI-H1703	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1703 cells Anticancer activity against human NCI-H1703 cells	[PMID: 34543572]
NCI-H1792	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1792 cells Anticancer activity against human NCI-H1792 cells	[PMID: 34543572]
NCI-H1793	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H1793 cells Anticancer activity against human NCI-H1793 cells	[PMID: 34543572]
NCI-H2009	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H2009 cells Anticancer activity against human NCI-H2009 cells	[PMID: 34543572]
NCI-H2030	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H2030 cells Anticancer activity against human NCI-H2030 cells	[PMID: 34543572]
NCI-H211	IC₅₀	0.3 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H211 cells Anticancer activity against human NCI-H211 cells	[PMID: 34543572]
NCI-H211	IC₅₀	5.6 nM Compound: 18; BMS-986158	Anticlonogenic activity against human NCI-H211 cells Anticlonogenic activity against human NCI-H211 cells	[PMID: 34543572]
NCI-H211	IC₅₀	6.57 nM Compound: 1; BMS-986158	Antiproliferative activity against human NCI-H211 cells assessed as reduction in cell viability by MTS assay Antiproliferative activity against human NCI-H211 cells assessed as reduction in cell viability by MTS assay	[PMID: 36893627]
NCI-H2170	IC₅₀	91 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H2170 cells Anticancer activity against human NCI-H2170 cells	[PMID: 34543572]
NCI-H2228	IC₅₀	166 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H228 cells Anticancer activity against human NCI-H228 cells	[PMID: 34543572]
NCI-H23	IC₅₀	62 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H23 cells Anticancer activity against human NCI-H23 cells	[PMID: 34543572]
NCI-H441	IC₅₀	118 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H441 cells Anticancer activity against human NCI-H441 cells	[PMID: 34543572]
NCI-H520	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H520 cells Anticancer activity against human NCI-H520 cells	[PMID: 34543572]
NCI-H647	IC₅₀	441 nM Compound: 18; BMS-986158	Anticancer activity against human NCI-H647 cells Anticancer activity against human NCI-H647 cells	[PMID: 34543572]
OCI-AML-3	IC₅₀	0.7 nM Compound: 18; BMS-986158	Anticancer activity against human OCI-AML3 cells Anticancer activity against human OCI-AML3 cells	[PMID: 34543572]
SK-LU-1	IC₅₀	210 nM Compound: 18; BMS-986158	Anticancer activity against human SK-LU-1 cells Anticancer activity against human SK-LU-1 cells	[PMID: 34543572]
SK-MES-1	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human SK-MES-1 cells Anticancer activity against human SK-MES-1 cells	[PMID: 34543572]
SW900	IC₅₀	>500 nM Compound: 18; BMS-986158	Anticancer activity against human SW900 cells Anticancer activity against human SW900 cells	[PMID: 34543572]

In Vitro

BMS-986158 is an inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BMS-986158 binds to the acetyl-lysine binding site in the BRD of BET proteins, thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth^[2].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1800340-40-2
Appearance Solid
Molecular Weight 495.62
Formel C₃₀H₃₃N₅O₂
Color White to off-white
SMILES

OC(C)(C)C1=CC=C2C(N([C@H](C3=CC=CC=C3)C4CCOCC4)C5=C2N=CC(C6=C(C)N=NN6C)=C5)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (4)

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Journal Impact Factor

J Med Chem

Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [Abstract]

2020 Jul 9;63(13):7186-7210. PMID: 32453591
Pharmaceuticals (Basel)

Bromodomain and Extra-Terminal Inhibitor BMS-986158 Reverses Latent HIV-1 Infection In Vitro and Ex Vivo by Increasing CDK9 Phosphorylation and Recruitment. [Abstract]

2022 Mar 10;15(3):338. PMID: 35337136
J Pharmacol Exp Ther

Reprogramming oncogenic mitochondria in pancreatic adenocarcinoma through BRD4 inhibition leads to programmed cell death. [Abstract]

2025 Nov;392(11):103751. PMID: 41232326
Harvard University

2026.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (50.44 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

2.0177 mL

10.0884 mL

20.1767 mL

5 mM

0.4035 mL

2.0177 mL

4.0353 mL

10 mM

0.2018 mL

1.0088 mL

2.0177 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Solubility: ≥ 2.5 mg/mL (5.04 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.04 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yin M, et al. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020 Apr 14;11(1):1833. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0177 mL	10.0884 mL	20.1767 mL	50.4419 mL
	5 mM	0.4035 mL	2.0177 mL	4.0353 mL	10.0884 mL
	10 mM	0.2018 mL	1.0088 mL	2.0177 mL	5.0442 mL
	15 mM	0.1345 mL	0.6726 mL	1.3451 mL	3.3628 mL
	20 mM	0.1009 mL	0.5044 mL	1.0088 mL	2.5221 mL
	25 mM	0.0807 mL	0.4035 mL	0.8071 mL	2.0177 mL
	30 mM	0.0673 mL	0.3363 mL	0.6726 mL	1.6814 mL
	40 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2610 mL
	50 mM	0.0404 mL	0.2018 mL	0.4035 mL	1.0088 mL

Keywords

BMS-986158

4 Cited Publications

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BMS-986158

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) BMS-986158

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-986158

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) BMS-986158

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-986158 Related Classifications

HY-101567 Related Classifications