ZM 39923 HCl

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

For research use only.

Catalog No.S8004

5 publications

CAS No. 1021868-92-7

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.

Selleck's ZM 39923 HCl has been cited by 5 publications

Carcinogenesis, 2020, 41(7):993-1004

PubMed: 31740922 ( click the link to review the publication )

Int J Biol Sci, 2019, 15(9):1882-1891

PubMed: 31523190 ( click the link to review the publication )

Cancer Sci, 2018, 109(12):3726-3736

PubMed: 30264546 ( click the link to review the publication )

Oncoimmunology, 2017, 6(11):e1353860

PubMed: 29147602 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2017, 114(6):E980-E989

PubMed: 28049849 ( click the link to review the publication )

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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

References

Solubility (25°C)

In vitro	DMSO	30 mg/mL (81.54 mM)
	Ethanol	8 mg/mL (21.74 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download ZM 39923 HCl SDF

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

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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JAK Signaling Pathway Map

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ZM 39923 HCl