I-BET151 dihydrochloride
Based on 30 publication(s) in Google Scholar
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
For research use only. We do not sell to patients.
- CAS No.: 1883545-47-8
- Formula: C23H23Cl2N5O3
- Molecular Weight:488.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) I-BET151 dihydrochloride
More- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Cell Stem Cell. 2021 Sep 2;28(9):1597-1613.e7. [Abstract]
- Nat Commun. 2026 Jun 17;17(1):5361. [Abstract]
- Sci Adv. 2025 Jul 11;11(28):eadv0079. [Abstract]
- Clin Cancer Res. 2025 Mar 3;31(5):907-920. [Abstract]
- J Transl Med. 2026 Feb 4;24(1):385. [Abstract]
- J Transl Med. 2022 Jul 28;20(1):336. [Abstract]
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Mater Today Chem. aterials Today Chemistry 12 (2019) 78e84
- Biochem Pharmacol. 2023 Apr:210:115497. [Abstract]
- Biochem Pharmacol. 2020 Oct:180:114126. [Abstract]
- Stem Cell Reports. 2017 Mar 14;8(3):538-547. [Abstract]
- PLoS Pathog. 2020 Mar 24;16(3):e1008429. [Abstract]
- J Mol Cell Cardiol. 2019 Feb:127:83-96. [Abstract]
- Oncol Rep. 2021 May;45(5):70. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- ACS Chem Neurosci. 2018 Dec 19;9(12):3175-3185. [Abstract]
- J Biol Chem. 2016 Nov 4;291(45):23756-23768. [Abstract]
- J Proteome Res. 2023 Sep 1;22(9):2880-2889. [Abstract]
- Front Oncol. 2021 Apr 16:11:656628. [Abstract]
- Anal Sens. 22 June 2022.
- Biochem Biophys Res Commun. 2022 Jan 15:588:147-153. [Abstract]
- Biochem Biophys Res Commun. 2021 Jun 18:558:216-223. [Abstract]
- bioRxiv. 2025 Aug 07.
- J Pers Med. 2024 Feb 20;14(3):224. [Abstract]
- Research Square Preprint. 2023 Jul 11.
- Brain Science Advances. 2022 Feb.
- bioRxiv. January 21, 2022.
- Patent. US20180263995A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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RT-PCR
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WB
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Flow Cytometry
Biological Activity
pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]
I-BET151 dihydrochloride (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 dihydrochloride (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.
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Cell Line:H929 cells
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Concentration:1 μM
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Incubation Time:72 hours
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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.
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Cell Line:H929 cells
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Concentration:100 nM
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Incubation Time:72 hours
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Result:Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.
I-BET151 dihydrochloride (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.
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Animal Model:Mice (model of subcutaneous myeloma)[2]
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Dosage:50 mg/kg
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Administration:I.p.; daily for 21 days
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Result:Reduced rate of tumor size doubling than vehicle-treated mice.
Chemical Information
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CAS No. 1883545-47-8
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Molecular Weight 488.37
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Formula C23H23Cl2N5O3
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SMILES
[H]Cl.[H]Cl.C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5
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Synonyms
GSK1210151A dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (30)
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Journal Impact Factor
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Most Recent
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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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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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 -
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
2021 Apr;40(15):2711-2724. PMID: 33712705 -
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 -
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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
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 -
Oncol Rep
BET inhibitors combined with chemotherapy synergistically inhibit the growth of NSCLC cells. [Abstract]2021 May;45(5):70. PMID: 33760217 -
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 -
ACS Chem Neurosci
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 -
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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 -
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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 -
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Purity & Documentation
References
[1]. Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. [Content Brief]
[2]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
I-BET151 dihydrochloride Related Classifications
HY-110106 Related Classifications
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