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TTP 22 Sale

(Synonyms: TTP22;TTP-22) 目录号 : GC10649

A CK2 inhibitor

TTP 22 Chemical Structure

Cas No.:329907-28-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥956.00
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10mg
¥746.00
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50mg
¥3,245.00
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Sample solution is provided at 25 µL, 10mM.

Description

IC50= 0.1 μM; Ki= 40 nM

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].

In vivo: So far, no animal in vivo study has been conducted for TTP 22.

Clinical trial: N/A

Reference:
[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.

化学性质

Cas No. 329907-28-0 SDF
别名 TTP22;TTP-22
化学名 3-[5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4-yl]sulfanylpropanoic acid
Canonical SMILES CC1=CC=C(C=C1)C2=CSC3=C2C(=NC=N3)SCCC(=O)O
分子式 C16H14N2O2S2 分子量 330.42
溶解度 ≥ 16.5 mg/mL in DMSO, ≥ 7.85 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 3.0265 mL 15.1323 mL 30.2645 mL
5 mM 0.6053 mL 3.0265 mL 6.0529 mL
10 mM 0.3026 mL 1.5132 mL 3.0265 mL
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