956025-83-5 Usage
Description
4-Amino-1-tert-butyl-3-(3-methylbenzyl)pyrazolo[3,4-d]pyrimidine is a cell-permeable C3-enlarged PP1 analog that acts as a potent, ATP-competitive, and highly ASKA-selective inhibitor against various kinases, including polo-like kinase 1, ZAP-70, and Syk. It is a white solid and is valuable in pharmacological validation of drug development and in elucidating enzyme signalings and functions when specific inhibitors against naturally occurring target enzymes are unavailable or difficult to generate.
Uses
Used in Pharmaceutical Industry:
4-Amino-1-tert-butyl-3-(3-methylbenzyl)pyrazolo[3,4-d]pyrimidine is used as a potent inhibitor for various kinases, such as polo-like kinase 1, ZAP-70, and Syk, for the development of drugs targeting these enzymes in the pharmaceutical industry.
Used in Research Applications:
4-Amino-1-tert-butyl-3-(3-methylbenzyl)pyrazolo[3,4-d]pyrimidine is used as a research tool to study the functions and signaling pathways of the targeted kinases in cell cultures and animal models, aiding in the understanding of their roles in various biological processes and diseases.
Used in Drug Development:
4-Amino-1-tert-butyl-3-(3-methylbenzyl)pyrazolo[3,4-d]pyrimidine is used as a lead compound in the development of new drugs targeting kinases involved in various diseases, such as cancer and inflammatory disorders, by providing a starting point for the design and optimization of more potent and selective inhibitors.
Biological Activity
3mb-pp1 is a cell-permeable, potent, atp-competitive, and highly selective inhibitor of polo-like kinase.human polo-like kinase 1 (plk1) plays dominant role in mitosis and the maintenance of genomic stability. plk1 is overexpressed in human tumours and exihibits prognostic potential in cancer, indicating its involvement in carcinogenesis and its potential as a therapeutic target [2].
in vitro
3mb-pp1 treatment significantly changed the dna state. in tbplkas cells, after treatment with 3mb-pp1 for 9 h, cells at all cell cycle stages showed an increase in detached new flagella when compared with vehicle control-treated samples [1]. the ic50 value of 3mb-pp1 against ptoas kinase activity was 120 nm. 3mb-pp1 was not able to significantly inhibit pti1 and mpk2. 3mb-pp1 significantly potentiated the interactions of ptoas with avrpto and avrptob1–387[3].
references
[1] lozano-núez a, ikeda k n, sauer t, et al. an analogue-sensitive approach identifies basal body rotation and flagellum attachment zone elongation as key functions of plk in trypanosoma brucei[j]. molecular biology of the cell, 2013, 24(9): 1321-1333.[2] strebhardt k, ullrich a. targeting polo-like kinase 1 for cancer therapy[j]. nature reviews cancer, 2006, 6(4): 321-330.[3] salomon d, bonshtien a, mayrose m, et al. bypassing kinase activity of the tomato pto resistance protein with small molecule ligands[j]. journal of biological chemistry, 2009, 284(22): 15289-15298.
Check Digit Verification of cas no
The CAS Registry Mumber 956025-83-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,5,6,0,2 and 5 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 956025-83:
(8*9)+(7*5)+(6*6)+(5*0)+(4*2)+(3*5)+(2*8)+(1*3)=185
185 % 10 = 5
So 956025-83-5 is a valid CAS Registry Number.
InChI:InChI=1/C17H21N5/c1-11-6-5-7-12(8-11)9-13-14-15(18)19-10-20-16(14)22(21-13)17(2,3)4/h5-8,10H,9H2,1-4H3,(H2,18,19,20)