THZ-P1-2 | PI5P4K inhibitor | Probechem Biochemicals

Chemical Structure : THZ-P1-2

CAS No.: 2058075-45-7

加入收藏

THZ-P1-2 (PI5P4K inhibitor THZ-P1-2)

货号: PC-38273Not For Human Use, Lab Use Only.

THZ-P1-2 is a potent, selective, covalent pan-PI5P4K inhibitor with IC50 of 190/700 nM for PI5P4Kα/β, respectively.

规格	价格	库存
5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

THZ-P1-2 is a potent, selective, covalent pan-PI5P4K inhibitor with IC50 of 190/700 nM for PI5P4Kα/β, respectively.
THZ-P1-2 exhibited 75% inhibition of PI-4,5-P2 formation PI5P4K γ at 0.7 uM.
THZ-P1-2 binds covalently to all isoforms of the PI5P4K family on unique cysteine residues located on a disordered loop outside the kinase domain.
THZ-P1-2 demonstrates cellular on-target engagement with limited off-targets across the kinome. PIKfyve is an off-target (IC50=40 nM) when used the commercially available DiscoverX KINOMEScan profiling platform.
THZ-P1-2 causes autophagosome clearance defects and upregulation in TFEB nuclear localization and target genes, disrupting autophagy in a covalent-dependent manner and phenocopying the effects of PI5P4K genetic deletion.
THZ-P1-2 is a useful tool to further interrogate the therapeutic potential of PI5P4K inhibition.

物理化学性质&存储条件

分子量	531.62
分子式	C31H29N7O2
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	(E)-N-(3-((6-(1H-Indol-3-yl)pyrimidin-4-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide

参考文献

1. Sindhu Carmen Sivakumaren, et al. Cell Chem Biol. 2020 May 21;27(5):525-537.e6.

THZ-P1-2 (PI5P4K inhibitor THZ-P1-2)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

THZ-P1-2 (PI5P4K inhibitor THZ-P1-2)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.