CAS:212844-53-6
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
Purvalanol A 是一种有效的 CDK 抑制剂。
Array ( [133] => Array ( [id] => 133 [name] => Inhibitors & Antagonists & Agonists [num] => 0 [children] => Array ( [352] => Array ( [id] => 352 [name] => Protein Tyrosine Kinase/PTK ) [350] => Array ( [id] => 350 [name] => PI3K/Akt/mTOR ) [351] => Array ( [id] => 351 [name] => Endocrinology & Hormones ) [357] => Array ( [id] => 357 [name] => Angiogenesis ) [358] => Array ( [id] => 358 [name] => HIF ) [363] => Array ( [id] => 363 [name] => Immunology & Inflammation ) [364] => Array ( [id] => 364 [name] => Stem Cells ) [365] => Array ( [id] => 365 [name] => Apoptosis ) [377] => Array ( [id] => 377 [name] => Metabolic Enzyme & Protease ) [379] => Array ( [id] => 379 [name] => Autophagy ) [380] => Array ( [id] => 380 [name] => ER Stress ) [384] => Array ( [id] => 384 [name] => Cell Cycle ) [385] => Array ( [id] => 385 [name] => Cytoskeleton ) [386] => Array ( [id] => 386 [name] => DNA Damage & DNA Repai ) [387] => Array ( [id] => 387 [name] => Epigenetics ) [388] => Array ( [id] => 388 [name] => Ubiquitin ) [389] => Array ( [id] => 389 [name] => JAK/STAT ) [390] => Array ( [id] => 390 [name] => GPCR & G Protein ) [391] => Array ( [id] => 391 [name] => Neuronal Signal Pathway ) [392] => Array ( [id] => 392 [name] => MAPK ) [393] => Array ( [id] => 393 [name] => NF-κB ) [394] => Array ( [id] => 394 [name] => Membrane Transporter & Ion Channel ) [395] => Array ( [id] => 395 [name] => TGF-β/Smad ) [396] => Array ( [id] => 396 [name] => Hippo ) [775] => Array ( [id] => 775 [name] => Antibody-drug Conjugate/ADC Related ) [122] => Array ( [id] => 122 [name] => Others ) ) ) )
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Purvalanol ACAS:212844-53-6
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
CAS | 212844-53-6 |
English Name | Purvalanol A |
Synonyms | NG-60;McN-JR3345;R3345;NG-60;2-(1R-ISOPROP; |
Molecular Formula | C19H25ClN6O |
Molecular Weight | 388.89 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | Light yellow to yellow Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD02179211 |
SMILES | CC([C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO)C |
Target Point | CDK |
Passage | Cell Cycle |
Background | Purvalanol A is a potent CDK inhibitor. |
Biological Activity | Purvalanol A 是一种有效的 CDK 抑制剂,对 cdc2-cyclin B,cdc2-cyclin B,cdk2-cyclin E,cdk4-cyclin D1 和 cdk5-p35 的 IC50 值分别为 4,70,35,850 和 75 nM。[1-3] |
IC50 | cdc2-cyclin B:4nM;cdk2-cyclin E:35nM;cdk2-cyclin A:70nM;cdk5-p35:75nM [1-3] |
In Vitro | Purvalanol A是CDK2的2.5倍强效抑制剂,但在低微摩尔范围内也有效抑制DYRK1A和许多其他蛋白激酶。 Purvalanol A抑制MKK1,MAPK2/ERK2,JNK/SAPK1c,IC50分别为80,26,84μM[2]。Purvalanol A抑制cdc28(酿酒酵母)和erk1,IC50为80和9000 nM。 Purvalanol A显示出针对60个人肿瘤细胞系的NCI组的抑制活性,平均GI50为2μM;两种细胞系对purvalanol A的敏感性增加~20倍:GI12为76 nM的KM12结肠癌细胞系和NCI-H522非小细胞肺癌细胞系,GI50为347 nM [1] 。 Purvalanol A选择性地抑制细胞蛋白的磷酸化。 Purvalanol A可防止血清诱导的G1期进展过程中细胞周期蛋白D和E含量的增加。 Purvalanol A在无细胞条件下不抑制转录[3]。 |
Data Literature Source | [1]. Gray NS,et al. Exploiting chemical libraries,structure,and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. [2]. Bain J,et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204. [3]. Villerbu N,et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9. |
Unit | Bottle |
Specification | 5mg 10mg 25mg |
Purvalanol A 是一种有效的 CDK 抑制剂。