Structure
I-BET762, Inhibitor
I-BET762
Purity
>98% (HPLC)
Synonyms
I-BET762; GSK525762A; GSK-525762A; I-BET-762; Molibresib; inhibitor
Purity/Purification
>98% (HPLC)
Suitability
10mM in DMSO
Target
Bromodomain
Receptor
BETproteins
Chemical Name
4H-[1, 2, 4]Triazolo[4, 3-a][1, 4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)
SMILES
O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
Molecular Formula
C22H22ClN5O2
CAS Number
1260907-17-2
Preparation and Storage
Store at -20 degree C
Stability: >=2 years
Shipping: Ice Pack
Stability: >=2 years
Shipping: Ice Pack
Structure
Structure
Related Product Information for I-BET762, inhibitor
I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF); inhibits binding of BET proteins to acetylated histones, disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, suppresses TNF-inducible key proinflammatory cytokine (il1b, il1a) and chemokine genes (ccl5, cxcl10, cxcl2/3) in BMDMs; inhibits the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in vivo in mouse model of EAE; inhibits myeloma cell proliferation both in vitro and myeloma xenograft models. Blood Cancer Phase 2 Clinical
Product Categories/Family for I-BET762, inhibitor
References
1. Nicodeme E, et al. Nature. 2010 Dec 23; 468 (7327):1119-23.
2. Bandukwala HS, et al. Proc Natl Acad Sci U S A. 2012 Sep 4; 109 (36):14532-7.
3. Mirguet O, et al. J Med Chem. 2013 Oct 10; 56 (19):7501-15.
4. Chaidos A, et al. Blood. 2014 Jan 30; 123 (5):697-705.
2. Bandukwala HS, et al. Proc Natl Acad Sci U S A. 2012 Sep 4; 109 (36):14532-7.
3. Mirguet O, et al. J Med Chem. 2013 Oct 10; 56 (19):7501-15.
4. Chaidos A, et al. Blood. 2014 Jan 30; 123 (5):697-705.
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Product Notes
The I-BET762 (Catalog #AAA3601080) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "I-BET762, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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