Molecular Formula | C23H26ClNO |
Molar Mass | 367.91164 |
Storage Condition | Inert atmosphere,Room Temperature |
In vitro study | ZM39923 decomposes to form the JAK3 inhibitor ZM449829 with similar IC50 values. In the presence of DTT(10 mM), the inhibitory effect of ZM39923 on TGM2 was reduced 300-fold. ZM39923 is a reversible inhibitor, and in the absence of Ca2, TGM2 is incubated with the inhibitor. ZM39923 significantly inhibited the crosslinking activity, and the IC50 was 25 nM in the absence of DTT and 10 μm in the presence of DTT. ZM39923 acts on the Drosophila Melanogaster model of polyglutamine repeat disorder to prevent premature death, a disease known as Machado-Joseph disease. ZM39923 inhibited the production of AICD-FLAG and Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent manner with an IC50 of about 20 μm. ZM39923 reduced photoaffinity labeling by PS1-CTF in the presence of γ-secretase. ZM39923 decomposes in neutral buffer, effectively inhibiting Janus kinase 3, and can be used as a standard Jak3 inhibitor in the experiment. |
biological activity | ZM 39923 HCl is a JAK1/3 inhibitor, pIC50 is 4.4/7.1, has no activity on JAK2, and acts moderately and effectively on EFGR; Sensitive to transglutaminase. |
in vitro study | ZM39923 decomposition to form JAK3 inhibitor ZM449829, with similar IC50 value. In the presence of DTT(10 mM), the effect of ZM39923 inhibiting TGM2 is reduced by 300 times. ZM39923 is a reversible inhibitor. In the absence of Ca2, TGM2 is incubated with the inhibitor. ZM39923 significantly inhibited cross-linking activity, IC50 was 25 nM in the absence of DTT and 10 μM in the presence of DTT. ZM39923 act on the Drosophila Melanogaster model of polyglutamine repeat disorder to prevent premature death, a disease called Machado-Joseph disease. ZM39923 the production of AICD-FLAG and Aβ40 and Aβ42 is inhibited by purified γ-secretase. This effect is concentration-dependent, and the IC50 is about 20 μM. ZM39923 reduces the PS1-CTF of photoaffinity markers in the presence of γ-secretase. ZM39923 is decomposed in neutral buffer to effectively inhibit Janus kinase 3, which can be used as a standard Jak3 inhibitor in the experiment. |
features | ZM39923 as a prodrug |
target | JAK3 7.1 (pIC 50 ) JAK1 4.4 (pIC 50 ) EGF-R 5.6 (pIC 50 ) Lck 5.0 (pIC 50 ) CDK4 5.0 (pIC 50 ) TGM2 10 nM (IC 50 ) |