BI-78D3
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1420 | Check With Us |
| 1g | $2130 | Check With Us |
: Cat #: V2665 CAS #: 883065-90-5 Purity ≥ 98%
Description: BI-78D3 (also known as JNK Inhibitor X) is a novel, potent and competitive JNK inhibitor with IC50 of 280nM.
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| Molecular Weight (MW) | 379.37 |
|---|---|
| Molecular Formula | C13H9N5O5S2 |
| CAS No. | 883065-90-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (263.6 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C1NN=C(SC2=NC=C([N+]([O-])=O)S2)N1C3=CC=C(OCCO4)C4=C3 |
| Synonyms | BI-78D3; BI78D3; BI 78D3; JNK Inhibitor X |
| Protocol | In Vitro | BI-78D3, dose-dependently inhibits the phosphorylation of JNK substrates both in vitro and in cell. BI-78D3 is able to compete with the D-domain of JIP1 (amino acids 153-163; pepJIP1) for JNK1 binding (IC50=500 nM). Using the same in vitro LanthaScreen kinase assay and the same ATF2 substrate, BI-78D3 is found to be 100-fold less active vs. p38α, a member of the MAPK family with high structural similarity to JNK, and completely inactive against mTOR and PI3-kinase (α-isoform), both unrelated protein kinases. Furthermore, Lineweaver-Burk analysis clearly indicates that BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In an attempt to profile the properties of BI-78D3 in the context of a complex cellular milieu, the cell-based LanthaScreen kinase assay is used. In this assay BI-78D3 is able to inhibit TNF-α stimulated phosphorylation of c-Jun in cell (EC50=12.4 μM). |
|---|---|---|
| In Vivo | The link between ConA-induced liver failure, TNF receptor signaling, and JNK function has been established by studies employing JNK1-/- and JNK2-/- mice. For this analysis, insulin insensitive mice are injected only once with 25 mg/kg BI-78D3, 30 min before insulin injection. The effect of insulin on blood glucose levels is then measured. BI-78D3 results in a statistically significant reduction in blood glucose levels as compared with the vehicle control. Thus, the ability of BI-78D3 to abrogate ConA-induced liver damage and restore insulin sensitivity is consistent with its proposed function as an effective JNK inhibitor. Liquid chromatography/mass spectrometry bio-availability analysis demonstrates that BI-78D3 has favorable microsome and plasma stability (T1/2=54 min). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6359 mL | 13.1797 mL | 26.3595 mL | 52.7190 mL |
| 5mM | 0.5272 mL | 2.6359 mL | 5.2719 mL | 10.5438 mL |
| 10mM | 0.2636 mL | 1.3180 mL | 2.6359 mL | 5.2719 mL |
| 20mM | 0.1318 mL | 0.6590 mL | 1.3180 mL | 2.6359 mL |
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