Plek2 inhibitor NUP-17d

Chemical Structure : Plek2 inhibitor NUP-17d

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货号: PC-49703Not For Human Use, Lab Use Only.

Plek2 inhibitor NUP-17d is a specific small molecule inhibitor of Pleckstrin-2 (Plek2), binds to Plek2 and Plek2-DEP with high affinity (ITC KD=109 and 350 nM, respectively).

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

Plek2 inhibitor NUP-17d is a specific small molecule inhibitor of Pleckstrin-2 (Plek2), binds to Plek2 and Plek2-DEP with high affinity (ITC KD=109 and 350 nM, respectively).
NUP-17d has IC50 of 7.8 µM in the erythroid in vitro proliferation assay.
NUP-17d also significantly inhibited enucleation and differentiation (at higher dosage) of the cultured erythroid cells and induced apoptosis.
NUP-17d is specific for Plek2, showed no inhibitory effect when Plek2 was acutely depleted by shRNA.
NUP-17d dramatically reverted lamellipodia in Plek2 overexpressed cells (Cos-7 cells), blocked Plek2-mediated Akt activation, induceed a confirmation change of Plek2 protein, which leads to Akt dissociation from the lipid-Plek2 complex and instability.
NUP-17d (25 mg/kg, 10% DMSO, 2% ethanol, 2% TWEEN80 and 86% 0.5% captisol) significantly reduced EPO-induced leukocytosis, reticulocytosis, extramedullary erythropoiesis, and vascular occlusions in the lungs of EPO injection models.
NUP-17d (25 mg/kg) reduced myeloproliferation in JAK2V617F models.
NUP-17d (25 mg/kg) demonstrated synergistic effects when combined with Akt inhibitor MK-2206 in human MPN cells.
Pleckstrin-2 (Plek2) is a downstream target of the JAK2-STAT pathway and overexpressed in patients with myeloproliferative neoplasms (MPNs), Plek2 activates Akt and protects Akt through Hsp72.

物理化学性质&存储条件

分子量	397.90
分子式	C22H24ClN3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(4-chlorophenyl)-2-hydroxy-1-(1H-indol-3-yl)-3-(4-methylpiperazin-1-yl)propan-1-one

参考文献

1. Xu Han, et al. J Clin Invest. 2023 Jan 31;e159638.