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(+)-JQ1 (1268524-70-4)

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2),binding to all bromodomains of the BET family, but not to bromodomains outside the BET family

Not Intended for Therapeutic Use. For research use only.

CAS: 1268524-70-4 Category

(+)-JQ1 (1268524-70-4) Description:

(+)-JQ1 is a BET potent BET bromodomain Inhibitor. Bromodomain and extra terminal domain (BET) proteins are important epigenetic regulators facilitating the transcription of genes in chromatin areas linked to acetylated histones. JQ1 has antiproliferative activity against many cancers, mainly through inhibition of c-MYC and upregulation of p21. JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer. JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models. JQ1 disrupts human dendritic cell maturation by inhibiting STAT5.

(+)-JQ1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin.

(+)-JQ1 (1268524-70-4) Specifications:

Product Name (+)-JQ1
Synonym (+)-JQ1; (+)-JQ-1; (+)-JQ 1; Bromodomain Inhibitor
Chemical Name tert-butyl (S)-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
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 1268524-70-4
Molecular Formula C23H25ClN4O2S
Molecular Weight 456.99
Monoisotopic Mass 456.13867  g/mol
MDL number MFCD22683748
InChIKey DNVXATUJJDPFDM-KRWDZBQOSA-N
InChi Code InChI=1S/C23H25ClN4O2S/c1-12-13(2)31-22-19(12)20(15-7-9-16(24)10-8-15)25-17(11-18(29)30-23(4,5)6)21-27-26-14(3)28(21)22/h7-10,17H,11H2,1-6H3/t17-/m0/s1
SMILES O=C(OC(C)(C)C)C[[email protected]]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
Form Powder
Color white to beige
Solubility  Soluble in DMSO 20 mg/mL, clear.
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A BET bromodomain inhibitor

 

 

 

RIDADR NONH for all modes of transport

References:

[1]. Kumar K, Raza SS, Knab LM, Chow CR, Kwok B, Bentrem DJ, Popovic R, Ebine K, Licht JD, Munshi HG. GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1. Sci Rep. 2015 Mar 25;5:9489. doi: 10.1038/srep09489. PubMed PMID: 25807524.

[2]. Qiu H, Jackson AL, Kilgore JE, Zhong Y, Chan LL, Gehrig PA, Zhou C, Bae-Jump VL. JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer. Oncotarget. 2015 Mar 30;6(9):6915-30. PubMed PMID: 25762632.

[3]. Toniolo PA, Liu S, Yeh JE, Moraes-Vieira PM, Walker SR, Vafaizadeh V, Barbuto JA, Frank DA. Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturation. J Immunol. 2015 Apr 1;194(7):3180-90. doi: 10.4049/jimmunol.1401635. Epub 2015 Feb 27. PubMed PMID: 25725100; PubMed Central PMCID: PMC4369449.

[4]. Ghurye RR, Stewart HJ, Chevassut TJ. Bromodomain inhibition by JQ1 suppresses lipopolysaccharide-stimulated interleukin-6 secretion in multiple myeloma cells. Cytokine. 2015 Feb;71(2):415-7. doi: 10.1016/j.cyto.2014.11.013. Epub 2014 Dec 4. PubMed PMID: 25482841.

[5]. Wang Y, Ma LM, Wang XZ, Wang T. [Mechanism of Notch1 Pathway in SUP-B15 Cell Apoptosis Induced by JQ1]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2015 Apr;23(2):364-8. doi: 10.7534/j.issn.1009-2137.2015.02.013. Chinese. PubMed PMID: 25948186.