ZM39923 HCl | ZM 39923 (hydrochloride) | JAK Inhibitor | AmBeed-信号通路专用抑制剂

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ZM 39923 盐酸盐 /ZM39923 HCl 97%

货号：A107403 同义名： ZM 39923 (hydrochloride);Janus-Associated Kinase 3 Inhibitor IV

ZM39923 HCl is a potent and selective JAK3 inhibitor with pIC50 value of 7.1, as well as inhibits EGFR, JAK1 and CDK4 with pIC50 values of 5.6, 4.4, and < 5.0.

ZM39923 HCl 化学结构
CAS号：1021868-92-7

ZM39923 HCl 3D分子结构
CAS号：1021868-92-7

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ZM39923 HCl 纯度/质量文件产品仅供科研

货号：A107403 标准纯度： 97% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

JAK 亚型比较

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, IC50: 11 nM JAK1, Ki: 11 nM	+++ JAK2, Ki: 13 nM	++++ JAK3, Ki: 2.5 nM	+++ TYK2, Ki: 13 nM		99%+
ZM39923 HCl	+ JAK1, pIC50: 4.4		+ JAK3, pIC50: 7.1		EGFR	97%
Cerdulatinib	+++ JAK1, IC50: 12 nM	+++ JAK2, IC50: 6 nM	+++ JAK3, IC50: 8 nM	++++ TYK2, IC50: 0.5 nM		99%+
Momelotinib	+++ JAK1, IC50: 11 nM	++ JAK2, IC50: 18 nM	+ JAK3, IC50: 155 nM			99%+
XL019	+ JAK1, IC50: 134.3 nM	++++ JAK2, IC50: 2.2 nM	+ JAK3, IC50: 214.2 nM		FLT3	99%+
Ruxolitinib	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM				98%
Tofacitinib	+ JAK1, IC50: 112 nM	++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			98%
Ruxolitinib (S enantiomer)	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM		++ TYK2, IC50: 19 nM		98%
Filgotinib	+++ JAK1, IC50: 10 nM	++ JAK2, IC50: 28 nM	+ JAK3, IC50: 810 nM	+ TYK2, IC50: 116 nM		99%
Baricitinib	+++ JAK1, IC50: 5.9 nM	+++ JAK2, IC50: 5.7 nM		++ TYK2, IC50: 53 nM		99%
Gandotinib	++ JAK1, IC50: 19.8 nM	++++ JAK2 (V617F), Ki: 0.245 nM JAK2, IC50: 0.288 nM	++ JAK3, IC50: 48.0 nM	++ TYK2, IC50: 44 nM	FLT3	99%+
Oclacitinib maleate	+++ JAK1, IC50: 10nM	++ JAK2, IC50: 18nM	+ JAK3, IC50: 99nM	+ TYK2, IC50: 84nM		98+%
NVP-BSK805 2HCl	++ JAK1, IC50: 31.63 nM	++++ JAK2, IC50: ~0.5 nM	++ JAK3, IC50: 18.68 nM	+++ TYK2, IC50: 10.76 nM		99+%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM			RET,FLT3	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, Ki: 0.45 nM JAK2, IC50: <3 nM				97%
GLPG0634 analog		✔				99%+
CEP-33779		++++ JAK2, IC50: 1.8 nM				99%+
FLLL32		+ JAK2, IC50: <5 μM				99%+
WHI-P154			+ JAK3, IC50: 1.8 μM		EGFR,VEGFR,Src	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		98%
TG101209		+++ JAK2, IC50: 6 nM	+ JAK3, IC50: 169 nM		RET,FLT3	99%+
AT9283		++++ JAK2, IC50: 1.2 nM	++++ JAK3, IC50: 1.1 nM			99%+
Pacritinib		++ JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM	+ JAK3, IC50: 520 nM	++ TYK2, IC50: 50 nM	FLT3	97%
Tofacitinib citrate		++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			99%
FM-381			++++ JAK3, IC50: 127 pM			98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ZM39923 HCl 生物活性

靶点	JAK1 JAK1, pIC50:4.4 JAK3 JAK3, pIC50:7.1
描述	Janus kinase 3 (JAK3) is a tyrosine kinase mainly expressed in lymphoid cells. ZM39923 hydrochloride is a potent JAK3 inhibitor with a pIC50 value of 7.1±0.3. However, it is a weak inhibitor for EGF-R and Janus kinase 1 with pIC50 values of 5.6 and 4.4, respectively. ZM39923 hydrochloride showed insignificant inhibitory effect against tyrosine kinases Lck and CDK4 with a pIC50 of less than 5.0.^[3] ZM39923 hydrochloride is also a potent inhibitor of tissue transglutaminase with an IC50 of 10nM.^[4] The CCL19-induced phosphorylation of JAK3 in PCI-37B cells was inhibited by 10µM ZM39923 compared with the group treated with CCL19 alone. In SCCHN cells, ZM39923 at 10µM significantly blocked CCL19-induced wound closure rate compared with the control group.^[5]
作用机制	ZM39923 hydrochloride is a potent inhibitor for both JAK3 and tissue transglutaminase.^[4]

ZM39923 HCl 参考文献

[1]Fraering PC, Ye W, et al. gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site. J Biol Chem. 2005 Dec 23;280(51):41987-96.

[2]Brown GR, Bamford AM, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9.

[3]Brown GR, Bamford AM, Bowyer J, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000;10(6):575-579. doi:10.1016/s0960-894x(00)00051-2

[4]Lai TS, Liu Y, Tucker T, et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008;15(9):969-978. doi:10.1016/j.chembiol.2008.07.015

[5]Zhang Z, Liu F, Li Z, Wang D, Li R, Sun C. Jak3 is involved in CCR7-dependent migration and invasion in metastatic squamous cell carcinoma of the head and neck. Oncol Lett. 2017;13(5):3191-3197. doi:10.3892/ol.2017.5861

ZM39923 HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.59mL

2.72mL

1.36mL

27.18mL

5.44mL

2.72mL

ZM39923 HCl 技术信息

CAS号	1021868-92-7
分子式	C₂₃H₂₆ClNO
分子量	367.912

别名	ZM 39923 (hydrochloride);Janus-Associated Kinase 3 Inhibitor IV;JAK3 Inhibitor IV;ZM39923 hydrochloride
运输	蓝冰

存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 45 mg/mL(122.31 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 1 mg/mL(2.72 mM)，配合低频超声助溶

动物实验配方

ZM 39923 盐酸盐 /ZM39923 HCl 97%

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