ZM 39923 HCl 1021868-92-7

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Molecular Weight:

367.91 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.


Biological 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.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	367.91
Formula	C23H25NO.HCl
CAS No.	1021868-92-7

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	30 mg/mL (81.54 mM)
		Water	<1 mg/mL (
		Ethanol	8 mg/mL (21.74 mM)
* <1 mg/ml means slightly soluble or 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 Name	1-Propanone, 3-[(1-methylethyl)(phenylmethyl)amino]-1-(2-naphthalenyl)-, hydrochloride (1:1)

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Product Categories : Epigenetics > JAK Inhibitor