Art. -Nr.: HY-13235

I-BET151

(Synonyms: GSK1210151A)

30 Cited Publications

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Based on 30 publication(s) in Google Scholar

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively.

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Reinheit: 99.47%
CAS. Nr.: 1300031-49-5
Formel: C₂₃H₂₁N₅O₃
Molecular Weight:415.44

Speicherung:

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

I-BET151 Chemical Structure

CAS. Nr.: 1300031-49-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (30)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively^[1]^[2].

IC₅₀ & Target

pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	1 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
HL-60	IC₅₀	890 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human HL-60 cells harboring N-RAS assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human HL-60 cells harboring N-RAS assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
HL-60	IC₅₀	195 nM Compound: I-BET151	Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]
HT-29	IC₅₀	0.945 μM Compound: 3, I-BET151	Growth inhibition of human HT-29 cells after 72 hrs by SRB assay Growth inhibition of human HT-29 cells after 72 hrs by SRB assay	[PMID: 25559428]
K562	IC₅₀	>100 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
K562	IC₅₀	>2000 nM Compound: 3, I-BET-151	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]
MEG-01	IC₅₀	25 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MEG-01 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human MEG-01 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
MM1.S	IC₅₀	0.299 μM Compound: 3, I-BET151	Growth inhibition of human MM1S cells after 72 hrs by SRB assay Growth inhibition of human MM1S cells after 72 hrs by SRB assay	[PMID: 25559428]
MOLM-13	IC₅₀	120 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
MOLM-13	IC₅₀	228 nM Compound: 3, I-BET-151	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	228 nM Compound: 5; I-BET151	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	167 nM Compound: I-BET151, GSK1210151A	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	26 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 21964340]
MV4-11	IC₅₀	0.119 μM Compound: 3, I-BET151	Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay	[PMID: 25559428]
MV4-11	IC₅₀	162 nM Compound: 3, I-BET-151	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	162 nM Compound: 5; I-BET151	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]
MV4-11	IC₅₀	126.9 nM Compound: I-BET151	Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]
NOMO-1	IC₅₀	15 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human NOMO-1 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human NOMO-1 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
PBMC	IC₅₀	0.16 μM Compound: I-BET151, GSK1210151A	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	0.13 μM Compound: I-BET151, GSK1210151A	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]
RS4-11	IC₅₀	192 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human RS4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human RS4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
THP-1	IC₅₀	134.2 nM Compound: I-BET151	Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]

In Vitro

I-BET151 (1 μM; 72 hours) treatment displays the majority of live cells resided in the G₀ phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation^[2].
I-BET151 (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G₂ phase^[2].

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

Cell Viability Assay^[2]

Cell Line:

H929 cells
Concentration:

1 μM
Incubation Time:

72 hours
Result:

Displays the majority of live cells resided in the G₀ phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

Cell Proliferation Assay^[2]

Cell Line:

H929 cells
Concentration:

100 nM
Incubation Time:

72 hours
Result:

Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G₂ phase.

In Vivo

I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)^[1].
I-BET151 (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice^[2].

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

Animal Model:

Mice (model of subcutaneous myeloma)^[2]
Dosage:

50 mg/kg
Administration:

I.p.; daily for 21 days
Result:

Reduced rate of tumor size doubling than vehicle-treated mice.

Chemical Information

CAS. Nr. 1300031-49-5
Appearance Solid
Molecular Weight 415.44
Formel C₂₃H₂₁N₅O₃
Color White to khaki
SMILES

C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5
Synonyms

GSK1210151A
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 (30)

All Cell Proliferation/Viability AssayWBRT-PCRFlow Cytometry

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Journal Impact Factor

Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Cell Stem Cell

CD276 expression enables squamous cell carcinoma stem cells to evade immune surveillance. [Abstract]

2021 Sep 2;28(9):1597-1613.e7. PMID: 33945793
Nat Commun

Induced pluripotent stem cell-derived models of malignant nerve sheath tumor progression mimic glial to neuro-mesenchymal transition and uncover therapeutic opportunities. [Abstract]

2026 Jun 17;17(1):5361. PMID: 42310314
Sci Adv

NLRP3 inflammasome-driven hemophagocytic lymphohistiocytosis occurs independent of IL-1β and IL-18 and is targetable by BET inhibitors. [Abstract]

2025 Jul 11;11(28):eadv0079. PMID: 40632844

I-BET151 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]

I-BET151 (5 μM; 3 h or overnight) inhibited LPS- and nigericin-mediated, NLRP3-driven pyroptosis of BMDMs.

I-BET151 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]

I-BET151 (5 μM; overnight) reduced ASC oligomerization in macrophages following nigericin treatment and consequently limited caspase-1, GSDMD, and IL-1β processing into their bioactive fragments, including the release of cleaved caspase-1 and IL-1β into the cell supernatant.

I-BET151 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]

I-BET151 (5 μM; overnight) prevented LPS-induced NLRP3 transcription and TLR-induced IL-1β transcription in BMDMs.

I-BET151 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]

I-BET151 (0.2-5 μM; overnight) limited the LPS– and Pam3CSK4–induced expression of NLRP3 and IL-1β in BMDMs.

I-BET151 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]

I-BET151 (5-10 μM; overnight) largely rescued the loss of macrophage viability following nigericin treatment.
Clin Cancer Res

Triple Combination of MEK, BET, and CDK Inhibitors Significantly Reduces Human Malignant Peripheral Nerve Sheath Tumors in Mouse Models. [Abstract]

2025 Mar 3;31(5):907-920. PMID: 39786423
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
J Transl Med

Personalized medicine strategy for MPNSTs: using precision oncology on PDOX models to inform tumor boards. [Abstract]

2026 Feb 4;24(1):385. PMID: 41639724
J Transl Med

The BRD4 inhibitor JQ1 suppresses tumor growth by reducing c-Myc expression in endometrial cancer. [Abstract]

2022 Jul 28;20(1):336. PMID: 35902869
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Mater Today Chem

aterials Today Chemistry 12 (2019) 78e84
Biochem Pharmacol

BRD4 promotes hepatic stellate cells activation and hepatic fibrosis via mediating P300/H3K27ac/PLK1 axis. [Abstract]

2023 Apr:210:115497. PMID: 36907496
Biochem Pharmacol

Macrophages confer resistance to BET inhibition in triple-negative breast cancer by upregulating IKBKE. [Abstract]

2020 Oct;180:114126. PMID: 32603665
Stem Cell Reports

Direct Generation of Human Neuronal Cells from Adult Astrocytes by Small Molecules. [Abstract]

2017 Mar 14;8(3):538-547. PMID: 28216149
PLoS Pathog

BRD4 inhibition exerts anti-viral activity through DNA damage-dependent innate immune responses. [Abstract]

2020 Mar 24;16(3):e1008429. PMID: 32208449
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
iScience

Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]

2024 May 16;27(6):110011. PMID: 38868181
Oncol Rep

BET inhibitors combined with chemotherapy synergistically inhibit the growth of NSCLC cells. [Abstract]

2021 May;45(5):70. PMID: 33760217
ACS Chem Neurosci

Direct Reprogramming of Glioblastoma Cells into Neurons Using Small Molecules. [Abstract]

2018 Dec 19;9(12):3175-3185. PMID: 30091580
J Biol Chem

Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases. [Abstract]

2016 Nov 4;291(45):23756-23768. PMID: 27650498
J Proteome Res

Quantitative Proteomics of the CDK9 Interactome Reveals a Function of the HSP90-CDC37-P-TEFb Complex for BETi-Induced HIV-1 Latency Reactivation. [Abstract]

2023 Sep 1;22(9):2880-2889. PMID: 37540094
Front Oncol

A Super-Enhancer Driven by FOSL1 Controls miR-21-5p Expression in Head and Neck Squamous Cell Carcinoma. [Abstract]

2021 Apr 16:11:656628. PMID: 33937067
Anal Sens

22 June 2022.
Biochem Biophys Res Commun

The CDK4/6-UCHL5-BRD4 axis confers resistance to BET inhibitors in MLL-rearranged leukemia cells by suppressing BRD4 protein degradation. [Abstract]

2022 Jan 15:588:147-153. PMID: 34954522
Biochem Biophys Res Commun

ATF2 inhibits ani-tumor effects of BET inhibitor in a negative feedback manner by attenuating ferroptosis. [Abstract]

2021 Jun 18:558:216-223. PMID: 33008584
bioRxiv

2025 Aug 07.
J Pers Med

Chromatin Remodeling-Related PRDM1 Increases Stomach Cancer Proliferation and Is Counteracted by Bromodomain Inhibitor. [Abstract]

2024 Feb 20;14(3):224. PMID: 38540967
Research Square Preprint

2023 Jul 11.
Brain Science Advances

2022 Feb.
bioRxiv

January 21, 2022.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (240.71 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

2.4071 mL

12.0354 mL

24.0709 mL

5 mM

0.4814 mL

2.4071 mL

4.8142 mL

10 mM

0.2407 mL

1.2035 mL

2.4071 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