329907-28-0

Basic information

• Product Name: TTP 22
• Synonyms: TTP 22;Propanoic acid, 3-[[5-(4-Methylphenyl)thieno[2,3-d]pyriMidin-4-yl]thio]-;3-[[5-(4-Methylphenyl)thieno[2,3-d]pyriMidin-4-yl]thio]propanoic acid;TTP 22 3-[[5-(4-Methylphenyl)thieno[2,3-d]pyrimidin-4-yl]thio]propanoic acid;TTP 22, >=98%;3-[2-(3-HYDROXY-5-METHOXYPHENYL)ETHYL]-6-METHOXY-2-(3-METHYL-2-BUTEN-1-YL)PHENOL
• CAS NO: 329907-28-0
• Molecular Formula: C₁₆H₁₄N₂O₂S₂
• Molecular Weight: 330.42456
• Product Categories: Inhibitors
• Mol File: 329907-28-0.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Storage Temp.: Keep in dark place,Sealed in dry,Store in freezer, under -20°C
• Solubility: insoluble in H2O; ≥16.5 mg/mL in DMSO; ≥7.85 mg/mL in EtOH with gentle warming and ultrasonic
• CAS DataBase Reference: TTP 22(CAS DataBase Reference)
• NIST Chemistry Reference: TTP 22(329907-28-0)
• EPA Substance Registry System: TTP 22(329907-28-0)

Safety Data

• Hazardous Substances Data: 329907-28-0(Hazardous Substances Data)

Usage

Uses

TTP 22 is a CK2 inhibitor.

Biological Activity

ttp 22 is a high affinity, atp-competitive casein kinase 2 (ck2) inhibitor.casein kinase 2 (ck2) noticeably stands out against a background of the kinase family due to its constitutive catalytic activity with the ability to phosphorylate more than 300 physiological substrates. these features make ck2 appear greatly diverse points of cell signaling pathways and be involved in processes leading to the development of various disorders, especially cancer. thus, currently ck2 is regarded as druggable protein kinase target and can be used for the development of antitumor, anti-inflammatory and antiviral drugs.

in vitro

kinetic studies of ttp 22 showed that activity of (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids moiety was a result of its competition with atp molecule for the binding site. inhibition constant (ki) for ttp 22 was 40 nm. initial in vitro tests of ttp 22 and it analog on four serine/threonine (ask1, jnk3, aurora a and rock 1) and three tyrosine protein kinases (fgfr1, met and tie2) revealed their remarkable specificity towards ck2 [1].

IC 50

= 0.1 μm; ki= 40 nm

references

[1] golub ag,bdzhola vg,briukhovetska nv,balanda ao,kukharenko op,kotey im,ostrynska ov,yarmoluk sm. synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase ck2. eur j med chem.2011 mar;46(3):870-6.

Upstream product

• 122-00-9 para-methylacetophenone 
• 15854-08-7 ethyl 2-amino-4-(4-methylphenyl)thiophene-3-carboxylate 
• 17509-21-6 5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4(3H)-one 
• 374104-63-9 4-chloro-5-(p-tolyl)thieno[2,3-d]pyrimidine 
• 107-96-0 3-mercaptopropionic acid 

Relevant articles and documents

Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin- 4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2

A novel series of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids has been synthesized and tested in vitro towards human protein kinase CK2. It was revealed that the most active compounds inhibiting CK2 are 3-{[5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4-yl]thio}propanoic acid and 3-{[5-(4-ethoxyphenyl)thieno[2,3-d]pyrimidin-4-yl]thio}propanoic acid (IC 50 values are 0.1 μM and 0.125 μM, respectively). Structure-activity relationships of 28 tested thienopyrimidine derivatives have been studied and binding mode of this chemical class has been predicted. Evaluation of the inhibitors on seven protein kinases revealed considerable selectivity towards CK2.