I-BET151 (Synonyms: GSK1210151A)

Name: I-BET151
Brand: MedChemExpress
SKU: HY-13235
Rating: 5.0 (26 reviews)

Cat. No.: HY-13235 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

I-BET151 Chemical Structure

CAS No. : 1300031-49-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 432	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 756	In-stock	Estimated Time of Arrival: December 31
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Based on 26 publication(s) in Google Scholar

Other Forms of I-BET151:

I-BET151 dihydrochloride Get quote

26 Publications Citing Use of MCE I-BET151

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Description

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]

Cellular Effect

Cell Line	Type	Value	Description	References
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	> 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]
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	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	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	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]
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]
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]
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.

Molecular Weight

415.44

Formula

C₂₃H₂₁N₅O₃

CAS No.

1300031-49-5

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 (6.02 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: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.02 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.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.20 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (286 KB) SDS (420 KB)

COA (260 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4071 mL	12.0354 mL	24.0709 mL	60.1772 mL
	5 mM	0.4814 mL	2.4071 mL	4.8142 mL	12.0354 mL
	10 mM	0.2407 mL	1.2035 mL	2.4071 mL	6.0177 mL
	15 mM	0.1605 mL	0.8024 mL	1.6047 mL	4.0118 mL
	20 mM	0.1204 mL	0.6018 mL	1.2035 mL	3.0089 mL
	25 mM	0.0963 mL	0.4814 mL	0.9628 mL	2.4071 mL
	30 mM	0.0802 mL	0.4012 mL	0.8024 mL	2.0059 mL
	40 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5044 mL
	50 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2035 mL
	60 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0030 mL
	80 mM	0.0301 mL	0.1504 mL	0.3009 mL	0.7522 mL
	100 mM	0.0241 mL	0.1204 mL	0.2407 mL	0.6018 mL

I-BET151 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

I-BET1511300031-49-5GSK1210151AEpigenetic Reader DomainBETbromodomainBRD4BRD2BRD3Inhibitorinhibitorinhibit

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I-BET151 (Synonyms: GSK1210151A)

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Other Forms of I-BET151:

I-BET151 Related Antibodies

26 Publications Citing Use of MCE I-BET151

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Purity & Documentation

References

Customer Review

I-BET151 Related Antibodies

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Complete Stock Solution Preparation Table

I-BET151 Related Classifications

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