Free shipping on all orders over $ 500

I-BET-762

Cat. No. M2190

All AbMole products are for research use only, cannot be used for human consumption.

I-BET-762 Structure
Synonym:

GSK525762

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
1mg USD 37  USD37 In stock
2mg USD 54  USD54 In stock
5mg USD 87  USD87 In stock
10mg USD 125  USD125 In stock
50mg USD 383  USD383 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

I-BET-762 (GSK525762) is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins. BET inhibitor I-BET-762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. I-BET-762 (GSK525762) was previously shown to suppress the production of proinflammatory proteins by macrophages and block acute inflammation in mice. Treatment of naive CD4(+) T cells with I-BET-762 during the first 2 d of differentiation had long-lasting effects on subsequent gene expression and cytokine production. The short 2-d treatment with I-BET-762 inhibited the ability of antigen-specific T cells, differentiated under Th1 but not Th17 conditions in vitro, to induce pathogenesis in an adoptive transfer model of experimental autoimmune encephalomyelitis. The suppressive effects of I-BET-762 on T-cell mediated inflammation in vivo were accompanied by decreased recruitment of macrophages, consistent with decreased GM-CSF production by CNS-infiltrating T cells.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Prev Res (2018). Figure 1. I-BET-762
Method gavaged
Cell Lines Female PyMT mice
Concentrations 60 mg/kg
Incubation Time 48 hrs
Results Treatment with I-BET 762 significantly (p<0.05) delayed the development of mammary tumors. The average time of the first palpable tumor increased from 13.1±0.8 weeks in the control group to 16.3±1.0 weeks with the I-BET 762 treatment
Protocol (for reference only)
Cell Experiment
Cell lines isolated CD4+ T cells
Preparation method CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk-old 2D2 transgenic mice by using Invitrogen Dynal Beads according to manufacturer’s protocols. The isolated CD4+ T cells were stimulated with platebound anti-CD3 and anti-CD28 antibodies alone (ThN conditions), or in the presence of anti-IL4 and IL-12 (Th1 conditions), IL-4 and anti-IL12 (Th2 conditions), IL-1β, IL-6, and IL-23 (Th17 conditions), or TGF-β (Treg conditions). Along with the cytokine mixtures were included either the Control-768 (GSK525768A) or I-BET-762 (GSK525762A) compounds. The cells are stimulated in these condition for 60–72 h and then harvested and expanded with DMEM media containing 10% (vol/vol) FBS, antibiotics, Lglutamine, and B-2ME. The cells were counted and reset to 0.5 × 106 cells per mL on days 3 and 4 after initial stimulation. Over the course of 5 d of T-cell culture and expansion, the compounds were diluted 12-fold relative to the starting concentrations. In case of Th1, Th2, and iTreg conditions, IL-2 was added to the media at a final concentration of 20 units per mL. On day 5 after initial activation, the cells were harvested and restimulated with PMA (10 nM) and ionomycin (1 μM) for 6 h. Brefeldin A (10 μg/mL) was added during the last 2 h of stimulation. Subsequently, the cells were fixed with 4% (wt/vol) paraformaldehyde in PBS for 15 min at 25 °C, washed in PBS, and permeabilized in saponin buffer [PBS, 0.5% saponin (Sigma), 1% (wt/vol) BSA, and 0.1% (wt/vol) sodium azide]. Intracellular staining was performed as described for indicated cytokines. In some experiments, cell surface staining was completed before fixation.
Concentrations 125, 250, 500nM
Incubation time 60-72h
Animal Experiment
Animal models LPS-induced endotoxic shock of C57BL/6 mice model
Formulation 20% beta-cyclodextrin, 2% DMSO in 0.9% saline
Dosages 30 mg/kg
Administration retro-orbital or tail vein injection
Chemical Information
Molecular Weight 423.9
Formula C22H22ClN5O2
CAS Number 1260907-17-2
Solubility (25°C) DMSO 90 mg/mL
1M HCl: 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Bandukwala HS, et al. Proc Natl Acad Sci U S A. Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors.

[2] Delmore JE, et al. Cell. BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

[3] Nicodeme E, et al. Nature. Suppression of inflammation by a synthetic histone mimic.

Related Epigenetic Reader Domain Products
dBRD9 dihydrochloride 

dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader.

BBC0403 

BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively.

BAY-155 

BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM.

FHT-1015 

FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM.

ISOX-DUAL 

ISOX-DUAL is a dual CBP/BRD4 inhibitor with IC50 values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: I-BET-762, GSK525762 supplier, Epigenetic Reader Domain, inhibitors, activators

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.