614849

TOPK/PBK Inhibitor, HI-TOPK-032

A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).

• 동의어(들): TOPK/PBK Inhibitor, HI-TOPK-032
• 실험식(Hill 표기법): C₂₀H₁₁N₅OS
• CAS Number: 487020-03-1
• Molecular Weight: 369.40
• MDL number: MFCD03286313
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 효능: 2 μM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: rust
• solubility: DMSO: 2.5 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• SMILES string: [s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2
• InChI: 1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)
• InChI key: BCSBXWKRZUPFHW-UHFFFAOYSA-N

설명

일반 설명

A cell-permeable, ATP competitive, reversible indolizinoquinoxalin derivative that acts as a specific inhibitor of T-LAK-cell-originated protein kinase (TOPK/PBK)(IC₅₀ = 2 µM). Does not affect the activities of ERK1, JNK1, and p38 MAP kinases. At higher concentrations (~ 5 µM) also inhibits MEK1 activity. Shown to suppress the proliferation of HCT116 colon cancer cell line and block tumor growth in colon cancer xenograft models in a dose-dependent manner. Diminishes TOPK activity only in cells over-expressing TOPK without significantly affecting cells with low levels of expression. Also shown to increase the expression of p53, active caspase-7, cleaved poly-ADP-Ribose polymerase, and increase the phosphorylation of Cdc2.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
TOPK/PBK

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.

Use only fresh DMSO for reconstitution.

기타 정보

Kim, D., et al. 2012, Cancer Res.72, 3060.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable