| BI 78D3Competitive JNK inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
BI 78D3 Dilution Calculator
calculate
BI 78D3 Molarity Calculator
calculate
| Cas No. | 883065-90-5 | SDF | Download SDF |
| Chemical Name | 4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-((5-nitrothiazol-2-yl)thio)-4H-1,2,4-triazol-3-ol | ||
| Canonical SMILES | OC1=NN=C(SC2=NC=C(S2)N(=O)=O)N1C3=CC4=C(OCCO4)C=C3 | ||
| Formula | C13H9N5O5S2 | M.Wt | 379.37 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
