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1,2,3,4,5,6-HexabromocyclohexaneJAK2 tyrosine kinase inhibitor

1,2,3,4,5,6-Hexabromocyclohexane

Catalog No. BCC2437
Size Price Stock
50mg $106.00 In stock
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Quality Control of 1,2,3,4,5,6-Hexabromocyclohexane

Chemical structure

1,2,3,4,5,6-Hexabromocyclohexane

Biological Activity of 1,2,3,4,5,6-Hexabromocyclohexane

Potently and directly inhibits JAK2 tyrosine kinase autophosphorylation, specifically inhibiting ligand-dependent JAK2 activation. A 16-hour treatment with 1 μM of compound reduces JAK2 tyrosine autophosphorylation levels to ~ 50% while 50 μM elimates nearly all JAK2 activity. Non-cytotoxic at 100 μM.

1,2,3,4,5,6-Hexabromocyclohexane Dilution Calculator

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1,2,3,4,5,6-Hexabromocyclohexane Molarity Calculator

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Chemical Properties of 1,2,3,4,5,6-Hexabromocyclohexane

Cas No. 1837-91-8 SDF Download SDF
Synonyms NSC 7908
Chemical Name 1,2,3,4,5,6-Hexabromocyclohexane
SMILES C1(C(C(C(C(C1Br)Br)Br)Br)Br)Br
Standard InChIKey QFQZKISCBJKVHI-UHFFFAOYSA-N
Standard InChI InChI=1S/C6H6Br6/c7-1-2(8)4(10)6(12)5(11)3(1)9/h1-6H
Formula C6H6Br6 M.Wt 557.54
Solubility Soluble to 10 mM in DMSO with gentle warming
Storage Store at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of 1,2,3,4,5,6-Hexabromocyclohexane

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7936 mL 8.968 mL 17.9359 mL 35.8719 mL 44.8398 mL
5 mM 0.3587 mL 1.7936 mL 3.5872 mL 7.1744 mL 8.968 mL
10 mM 0.1794 mL 0.8968 mL 1.7936 mL 3.5872 mL 4.484 mL
50 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.7174 mL 0.8968 mL
100 mM 0.0179 mL 0.0897 mL 0.1794 mL 0.3587 mL 0.4484 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Background on 1,2,3,4,5,6-Hexabromocyclohexane

Potently and directly inhibits JAK2 tyrosine kinase autophosphorylation, specifically inhibiting ligand-dependent JAK2 activation. A 16-hour treatment with 1 μM of compound reduces JAK2 tyrosine autophosphorylation levels to ~ 50% while 50 μM elimates nearly all JAK2 activity. Non-cytotoxic at 100 μM.

References on 1,2,3,4,5,6-Hexabromocyclohexane

Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of jak2 tyrosine kinase autophosphorylation [correction of autophophorylation].[Pubmed: 15801842]


The commercially available Jak2 inhibitor, alpha-cyano-3,4-dihydroxy-N-benzylcinnamide (AG490), has been used extensively to study Jak2 kinase function. While alpha-cyano-3,4-dihydroxy-N-benzylcinnamide is a potent Jak2 inhibitor, it can inhibit a number of other kinase signaling pathways as well. To circumvent this problem, we sought to identify novel small molecule inhibitors of Jak2 tyrosine kinase activity. For this, we constructed a homology model of the Jak2 kinase domain and identified solvent accessible pockets on the surface of the structure. Using the DOCK program, we tested 6451 compounds of known chemical structure in silico for their ability to interact with a pocket positioned adjacent to the activation loop. We attained the top seven scoring compounds from the National Cancer Institute and tested their ability to inhibit Jak2 autophosphorylation in vitro. Using Western blot analysis, we found that one of the compounds, 1,2,3,4,5,6-hexabromocyclohexane, was able to potently, and directly, inhibit Jak2 autophosphorylation. Characterization of this compound revealed that it inhibits Jak2 tyrosine autophosphorylation in both a time- and concentration-dependent manner. It greatly reduced growth hormone-mediated Jak2 autophosphorylation but did not block autophosphorylation of the epidermal growth factor receptor. Furthermore, doses as high as 100 muM were not toxic to cells as measured by their ability to exclude propidium iodide. As such, we believe that this compound could serve as a lead compound for a new generation of Jak2 inhibitors and, perhaps, be useful in elucidating the mechanisms of Jak2 kinase function.

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