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I-BET762
CAS No. 1260907-17-2
I-BET762 ( GSK525762A;GSK-525762A;I-BET-762;Molibresib )
Catalog No. M11080 CAS No. 1260907-17-2
I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 47 | In Stock |
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| 5MG | 77 | In Stock |
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| 10MG | 114 | In Stock |
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| 25MG | 205 | In Stock |
|
| 50MG | 339 | In Stock |
|
| 100MG | 507 | In Stock |
|
| 200MG | 713 | In Stock |
|
| 500MG | 1107 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameI-BET762
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NoteResearch use only, not for human use.
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Brief DescriptionI-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins.
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DescriptionI-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, 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
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SynonymsGSK525762A;GSK-525762A;I-BET-762;Molibresib
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PathwayChromatin/Epigenetic
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TargetBromodomain
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RecptorBETproteins
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1260907-17-2
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Formula Weight423.90
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Molecular FormulaC22H22ClN5O2
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
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Chemical Name4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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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