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ZM 39923 HCl

Name: ZM 39923 HCl
Brand: Selleck Chemicals
SKU: S8004
Rating: 5 (6 reviews)

Catalog No.S8004

For research use only.

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.

CAS No. 1021868-92-7

Selleck's ZM 39923 HCl has been cited by 6 Publications

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JAK Signaling Pathway Map

Biological Activity

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.

Features

ZM39923 acts as a prodrug.

Targets

TGM2 ^[2]	JAK3 ^[1]	EGFR ^[1]	JAK1 ^[1]
10 nM	7.1(pIC50)	5.6(pIC50)	4.4(pIC50)

In vitro

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. ^[1] 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. ^[2] 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. ^[3]

Protocol (from reference)

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	367.91
Formula	C₂₃H₂₅NO.HCl
CAS No.	1021868-92-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(C)N(CCC(=O)C1=CC2=CC=CC=C2C=C1)CC3=CC=CC=C3.Cl

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Handling Instructions

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