(+)-JQ-1 [1268524-70-4]

Catalog number: HY-13030_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 250.20 € 278.00
Expected delivery time: 10 days
Quantity:

Product specifications for - (+)-JQ-1 [1268524-70-4]

Overview: 
Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 1268524-70-4
Properties: 
Purity: >98%
Molecular Formula: C23H25ClN4O2S
Molecular weight: 456.9882
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2). IC50 Value: 77 nM(for BRD4(1)), 33 nM( for BRD4(2)) Target: BRD4 in vitro: (+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. in vivo: (+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts.
Safety information: 
MSDS: MSDS
Additional information: 
Synonyms: HY-13030; JQ-1; JQ1
Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk', Sdelci S. Nat Chem Biol. 2016 Jul;12(7):504-10. Read more
Bromodomain and extraterminal protein inhibition blocks growth of triple-negative breast cancers through the suppression of Aurora kinases.', Sahni JM. J Biol Chem. 2016 Nov 4;291(45):23756-23768. Read more
An Epigenetic Compound Library Screen Identifies BET Inhibitors That Promote HSV-1 and-2 Replication by Bridging P-TEFb to Viral Gene Promoters through BRD4', K Ren. PLoS Pathog. 2016 Oct 20;12(10):e1005950. Read more
The BET Bromodomain Inhibitor JQ1 Suppresses Chondrosarcoma Cell Growth via Regulation of YAP/p21/c-Myc Signaling.', Huan Tian Zhang. J Cell Biochem. 2017 Aug;118(8):2182-2192. Read more
Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia', Peirs S. Leukemia. 2017 Oct;31(10):2037-2047. Read more
Resveratrol Reactivates Latent HIV through Increasing Histone Acetylation and Activating Heat Shock Factor 1', Zeng X. J Agric Food Chem. 2017 Jun 7;65(22):4384-4394. Read more
Impact of target warhead and linkage vector on inducing protein degradation: comparison of Bromodomain and Extra-Terminal (BET) degraders derived from triazolodiazepine (JQ1) and tetrahydroquinoline (I-BET726) BET inhibitor scaffolds', Chan KH. J Med Chem. 2017 Jun 22. Read more
Glioblastoma cellular cross-talk converges on NF-κB to attenuate EGFR inhibitor sensitivity', Zanca C. Genes Dev. 2017 Jul 19. Read more
Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma—an aggressive and fatal disease', Stirnweiss A. Oncotarget. 2017 Dec 2;8(68):112313-112329. Read more
Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway', Wang L. Cell Death Dis. 2018 Jan 26;9(2):129. Read more