product name ZM 39923
Description: ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. When tested with RA cells, administration of ZM 39923 combined with 50 μg/ml curcumol suppressed CD4(+) T cell proliferation and induced apoptosis through inhibiting Jak3-STAT5-related molecular activities and Bcl-2 expression, respectively. In confluent ARPE-19 cells, pretreated with ZM 39923 followed acrolein treatment resulted in the reduction of cell viability and increased VEGF expression via mediating JAK3 and TGFβ2.
References: Chem Biol. 2008 Sep 22;15(9):969-78; J Biol Chem. 2005 Dec 23;280(51):41987-96.
367.91
Formula
C23H25NO.HCl
CAS No.
1021868-92-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 30 mg/mL (81.5 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (21.7 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: ZM39923 breaks down to form the JAK3 inhibitor ZM449829 which exhibit similar IC50 values. ZM39923 decomposes in neutral buffer to afford potent inhibition of the Janus kinase 3, and could be used as a standard Jak3 inhibitor in assays where breakdown could occur. ZM39923 is reduced by 300-fold in the presence of DTT (10 mM) in inhibiting TGM2. ZM39923 is reversible inhibitors when TGM2 is incubated with inhibitors in the absence of Ca2+. ZM39923 shows significant inhibition of crosslinking activity with IC50 of 25 nM in the absence of DTT and IC50 of 10 μM in the presence of DTT. ZM39923 prevents early death in a Drosophila Melanogaster model of a polyQ repeat disorder called Machado-Joseph Disease. ZM39923 inhibits the generation of AICD-FLAG and both Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent fashion with an approximate IC50 of 20 μM. ZM39923 decreases photoaffinity-labeled PS1-CTF in the presense of γ-secretase. Kinase Assay: Cell Assay: ZM39923 is a JAK3 inhibitor. ZM39923 is also a potent inhibitor of TGM2 with IC50 of 10 nM. ZM39923 is reversible inhibitors when TGM2 is incubated with inhibitors in the absence of Ca2+. ZM39923 shows significant inhibition of crosslinking activity with IC50 of 25 nM in the absence of DTT and IC50 of 10 μM in the presence of DTT. ZM39923 prevents early death in a Drosophila Melanogaster model of a polyQ repeat disorder called Machado-Joseph Disease. ZM39923 inhibits the generation of AICD-FLAG and both Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent fashion with an approximate IC50 of 20 μM. ZM39923 decreases photoaffinity-labeled PS1-CTF in the presense of γ-secretase. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Chem Biol. 2008 Sep 22;15(9):969-78; J Biol Chem. 2005 Dec 23;280(51):41987-96. |
