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(+)-JQ1, Tocris Bioscience™

Catalog No. 449910
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Quantity:
10 mg
This item is not returnable. View return policy
This item is not returnable. View return policy

Description

Potent and selective BET bromodomain inhibitor; cell permeable

(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively). (+)-JQ1 induces squamous differentiation in NUT midline carcinoma (NMC) cell lines and inhibits tumor growth in NMC xenograft models in vivo. (+)-JQ1 inhibits proliferation and induces autophagy in bladder cancer cells in vitro and in vivo. It also suppresses MYC gene expression and inhibits proliferation of lymphoma and leukemia cell lines. In human pulmonary microvasular endothelial cells (HPMEC), NF-κB activation, IL-6 and IL-8 expression and proliferation are inhibited by (+)-JQ1. The compound also inhibits transcription of ACE2 and TMPRSS2 genes in mouse lung tissue and prevents infection by SARS-CoV-2. In germ cells from male mice, (+)-JQ1 exhibits reversible contraceptive effects. (+)-JQ1 inhibits the BRD4-JUN-CCL2 axis in pancreatic cancer cells and improves survival by reducing macrophage recruitment.

Inactive Analog also available.

Carboxylic acid-functionalized (Cat. No. 6588) and click-activated (alkyne) (Cat. No. 6589) versions for PROTAC development also available.

Chemical Identifiers

CAS 1268524-70-4
Molecular Formula C23H25ClN4O2S
Molecular Weight (g/mol) 456.989
InChI Key DNVXATUJJDPFDM-KRWDZBQOSA-N
Synonym +-jq-1, +-jq1, jq1 compound, jq-1, unii-1mrh0imx0w, s-tert-butyl 2-4-4-chlorophenyl-2,3,9-trimethyl-6h-thieno 3,2-f 1,2,4 triazolo 4,3-a 1,4 diazepin-6-yl acetate, s-jq1, 1mrh0imx0w, jq1, bromodomain inhibitor, +-jq1
PubChem CID 46907787
SMILES CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C

Specifications

Quantity 10 mg
Formula Weight 456.99
Percent Purity >98%
Chemical Name or Material (+)-JQ1

Safety and Handling

Recommended Storage Store at -20°C
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