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JQ1 Enantiomers Set ((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, SGCBD01, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I)
A cell-permeable I-BET class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET family members BRD2, BRD3, BRD4, and BRD6/BRDT in a Kac- (epsilon-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT fusion-dependent NUT midline carcinoma and c-Myc oncoprotein-dependent multiple myeloma proliferation both in cultures (IC50 <1uM) in vitro and in mice (50mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively block BRDT-mediated spermatogenesis without affecting hormone levels. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1set. US Biological Life Sciences.
(+)-JQ1 carboxylic acid is the carboxylic acid form of BET bromodomain inhibitor (+)-JQ1. Synonyms: JQ-1 carboxylic acid; (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)acetic acid. Grades: ≥98%. CAS No. 202592-23-2. Molecular formula: C19H17ClN4O2S. Mole weight: 400.881.
(+)-JQ1 PA
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 2115701-93-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112789.
(R)-(-)-JQ1
(R)-(-)-JQ1 is the R-isomer and an inactive control of JQ1, a BET bromodomain inhibitor. Synonyms: (-)-JQ1; (-)-JQ 1; (-)-JQ-1; (R)-JQ1; (R)-(-)-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. Grades: >95%. CAS No. 1268524-71-5. Molecular formula: C23H25ClN4O2S. Mole weight: 456.989.
(R)-(-)-JQ1 Enantiomer
(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect. Uses: Scientific research. Group: Signaling pathways. CAS No. 1268524-71-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13030A.
(Z)-JQ1-TCO
JQ1-TCO (JQ1- trans -cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2087490-43-3. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-148864A.
AT 1
AT 1 is a highly selective BRD4 protein degrader composed of a BET bromodomain inhibitor (+)-JQ1 conjugated to a von Hippel-Lindau (VHL) ligand. Synonyms: BRD4 degrader AT1; (2S,4R)-1-((R)-2-acetamido-3-((6-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)hexyl)thio)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide. Grades: ≥98%. CAS No. 2098836-45-2. Molecular formula: C48H58ClN9O5S3. Mole weight: 972.68.
CeMMEC13
CeMMEC13 is an isoquinolinone and a potent inhibitor of TAF1 bromodomain with IC50 of 2.1 μM. It acts on the bromodomain of TAF1 but does not bind to bromodomains of BRD4, BRD9, or CREBBP. CeMMEC13 synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells. Synonyms: CeMMEC13; 1790895-25-8; 1-Methyl-2-oxo-1,2-dihydro-quinoline-4-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)-amide; N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-methyl-2-oxo-1,2-dihydroquinoline-4-carboxamide; CHEMBL4871450; N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-methyl-2-oxoquinoline-4-carboxamide; SCHEMBL20942221; BCP25037; EX-A1816; BDBM50572136; s8329; AKOS027600530; CeMMEC13, >=98% (HPLC); CCG-267868; AC-35506; BS-15617; HY-101088; CS-0020799; C73404; A924884; Z441586532; N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,2-dihydro-1-methyl-2-oxo-4-quinolinecarboxamide. Grades: ≥98%. CAS No. 1790895-25-8. Molecular formula: C19H16N2O4. Mole weight: 336.3.
dBET1
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1799711-21-9. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-101838.
(+)-JQ-1
BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Group: Biochemicals. Alternative Names: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic Acid 1,1-Dimethylethyl Ester; (+)-JQ1; (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. Grades: Highly Purified. CAS No. 1268524-70-4. Pack Sizes: 5mg, 10mg, 25mg, 50mg, 100mg. Molecular Formula: C??H??ClN?O?S, Molecular Weight: 456.99. US Biological Life Sciences.
Worldwide
(+)-JQ-1
(+)-JQ-1 is a potent and selective BET bromodomain inhibitor, IC50 values are 77 nM and 33 nM for inhibiting BRD4 (N-terminal) and BRD4 (C-terminal), respectively. Synonyms: JQ1. CAS No. 1268524-70-4. Molecular formula: C23H25ClN4O2S. Mole weight: 456.99.
(+)-JQ-1
(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: JQ1. CAS No. 1268524-70-4. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg; 500 mg. Product ID: HY-13030.
NH2-PEG3
NH2-PEG3 (PROTAC Linker 35) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. NH2-PEG3 (PROTAC Linker 35) can be used in the synthesis of the PROTAC (β-NF-JQ1) [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PROTAC Linker 35. CAS No. 6338-55-2. Pack Sizes: 1 g; 5 g. Product ID: HY-W007545.
NICE-01
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AP1867-PEG2-JQ1; AP-PEG2-JQ1. CAS No. 2982819-94-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg. Product ID: HY-156214.
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