1. Epigenetics
  2. Epigenetic Reader Domain

I-BET151 (Synonyms: GSK1210151A; I-BET 151; GSK-1210151A; GSK 1210151A)

Cat. No.: HY-13235 Purity: 98.47%
Handling Instructions

I-BET151 is a BET bromodomain inhibitor, 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

I-BET151 Chemical Structure

CAS No. : 1300031-49-5

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $120 In-stock
50 mg $360 In-stock
100 mg $630 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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

IC50 & Target

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

In Vitro

I-BET151 (GSK1210151A) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase at 24, 48, and 72 hours. The most pronounced effect is observed at 72 hours in all 6 myeloma cell lines, starting at 100 nM. Dual Ki67/propidium iodide staining confirmed that the majority of live cells resided in the G0 phase after treatment with I-BET151 at 1 μM for 72 hours commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].

In Vivo

I-BET151 (GSK1210151A) 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]. In an in vivo model of subcutaneous myeloma, I-BET151 (50 mg/kg)-treated mice has four- to five fold smaller myeloma tumors (P<0.001) and a significantly reduced rate of tumor size doubling than vehicle-treated mice (P<0.001)[2].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[2]

I-BET151 (GSK1210151A) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

For in vitro cell proliferation and apoptosis assays, myeloma cell lines are cultured by using RPMI 1640 medium supplemented with 10% fetal bovine serum, 2 mM L-glutamine, penicillin 500 IU/mL, and streptomycin 500 μg/mL. Cells are placed in 96-well U-bottom plates at final concentration of 0.2×106 cells per milliliter in a humidified incubator with 5% CO2 at 37°C. For stroma vs nonstroma experiments, myeloma cells are placed in flat-bottom 96-well plates with MS5 cells at >90% confluence or in wells without stroma. Compounds (ie, I-BET151, I-BET762, the inactive isomer I-BET768, and JQ1) are serially diluted into media and added to the cultures at the indicated concentrations, starting from a 10-mM DMSO stock solution. Primary myeloma cells are cultured in flat-bottom 96-well plates in the presence of MS5 stroma cells by using complete medium as above, supplemented with interleukin-6 (IL-6) at 5 ng/mL[2].

Animal Administration
[2]

I-BET151 (GSK1210151A) is dissolved in 0.9% NaCl plus Kleptose hydroxypropyl betadex 10% (w/v) (Mice)[2].

Mice[2]
NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice are used. In total, 5×106 KMS11 myeloma cells are injected subcutaneously into 9- to 12-week-old NSG mice. When tumors are ≥5 mm in maximum diameter, mice are randomized to receive once daily intraperitoneal injection of either I-BET151 30 mg/kg in 0.9% NaCl plus Kleptose hydroxypropyl betadex 10% (w/v) and DMSO 5% (v/v) pH 5.0 or vehicle solution for a maximum of 21 days.

References
M.Wt

415.44

Formula

C₂₃H₂₁N₅O₃

CAS No.

1300031-49-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 98.47%

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I-BET151
Cat. No.:
HY-13235
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