BI 78D3Competitive JNK inhibitor CAS# 883065-90-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 883065-90-5 | SDF | Download SDF |
| PubChem ID | 2747117 | Appearance | Powder |
| Formula | C13H9N5O5S2 | M.Wt | 379.37 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (263.59 mM; Need ultrasonic) | ||
| Chemical Name | 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-1,2,4-triazol-5-one | ||
| SMILES | C1COC2=C(O1)C=CC(=C2)N3C(=O)NN=C3SC4=NC=C(S4)[N+](=O)[O-] | ||
| Standard InChIKey | QFRLDZGQEZCCJZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H9N5O5S2/c19-11-15-16-12(25-13-14-6-10(24-13)18(20)21)17(11)7-1-2-8-9(5-7)23-4-3-22-8/h1-2,5-6H,3-4H2,(H,15,19) | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Competitive c-Jun N-terminal kinase (JNK) inhibitor (IC50 = 280 nM) that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. Inhibits JNK interacting protein 1 (JIP1)-JNK binding (IC50 = 500 nM) and prevents JNK substrate phosphorylation. Blocks JNK-dependent Con A-induced liver damage and restores insulin sensitivity in a mouse model of type II diabetes. |
BI 78D3 Dilution Calculator
BI 78D3 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6359 mL | 13.1797 mL | 26.3595 mL | 52.719 mL | 65.8987 mL |
| 5 mM | 0.5272 mL | 2.6359 mL | 5.2719 mL | 10.5438 mL | 13.1797 mL |
| 10 mM | 0.2636 mL | 1.318 mL | 2.6359 mL | 5.2719 mL | 6.5899 mL |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.0544 mL | 1.318 mL |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.5272 mL | 0.659 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. | |||||
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BI-78D3 is a substrate competitive inhibitor of JNK inhibitor [2].
JNK is a member of the MAPK family. JNK is a stress-activated protein kinase that modulates pathways implicated in a variety of disease states. Non-motoric JNK functions may differ between cell types and organs. The JNK is involved in a1-adrenoceptor-mediated contraction of prostate smooth muscle. For non-malignant, epithelial human prostate cells, JNK activation not only has the function of pro-apoptotic and antiproliferative but also related with JNK-dependent survival.[1]
BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In addition, it has been reported that BI-78D3 does not inhibit the phosphorylation of a short peptide substrate lacking a D-domain. This confirms that BI-78D3 is substrate competitive.[2]
BI-78D3 inhibits both noradrenaline- and phenylephrine-induced contractions. Then it prevents α1-adrenoceptor-mediated contraction of prostate tissue. As an effective JNK inhibitor, BI-78D3 has the ability of abrogating ConA-induced liver damage and restoring insulin sensitivity. [1,2]
References:
[1] Strittmatter F1, Walther S, Gratzke C, etal. , Inhibition of adrenergic human prostate smooth muscle contraction by the inhibitors of c-Jun N-terminal kinase, SP600125 and BI-78D3. Br J Pharmacol. 2012 Jul;166(6):1926-35.
[2] Stebbins JL, De SK, Machleidt T,etal. , Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.
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Inhibition of adrenergic human prostate smooth muscle contraction by the inhibitors of c-Jun N-terminal kinase, SP600125 and BI-78D3.[Pubmed:22364229]
Br J Pharmacol. 2012 Jul;166(6):1926-35.
BACKGROUND AND PURPOSE alpha(1) -Adrenoceptor-induced contraction of prostate smooth muscle is mediated by calcium- and Rho kinase-dependent mechanisms. In addition, other mechanisms, such as activation of c-jun N-terminal kinase (JNK) may be involved. Here, we investigated whether JNK participates in alpha(1)-adrenoceptor-induced contraction of human prostate smooth muscle. EXPERIMENTAL APPROACH Prostate tissue was obtained from patients undergoing radical prostatectomy. Effects of the JNK inhibitors SP600125 (50 microM) and BI-78D3 (30 microM) on contractions induced by phenylephrine, noradrenaline and electric field stimulation (EFS) were studied in myographic measurements. JNK activation by noradrenaline (30 microM) and phenylephrine (10 microM), and the effects of JNK inhibitors of c-Jun phosphorylation were assessed by Western blot analyses with phospho-specific antibodies. Expression of JNK was studied by immunohistochemistry and fluorescence double staining. KEY RESULTS The JNK inhibitors SP600125 and BI-78D3 reduced phenylephrine- and noradrenaline-induced contractions of human prostate strips. In addition, SP600125 reduced EFS-induced contraction of prostate strips. Stimulation of prostate tissue with noradrenaline or phenylephrine in vitro resulted in activation of JNK. Incubation of prostate tissue with SP600125 or BI-78D3 reduced the phosphorylation state of c-Jun. Immunohistochemical staining demonstrated the expression of JNK in smooth muscle cells of human prostate tissue. Fluorescence staining showed that alpha(1A)-adrenoceptors and JNK are expressed in the same cells. CONCLUSIONS AND IMPLICATIONS Activation of JNK is involved in alpha(1)-adrenoceptor-induced prostate smooth muscle contraction. Models of alpha(1)-adrenoceptor-mediated prostate smooth muscle contraction should include this JNK-dependent mechanism.
