N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
- Product Name
- N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
- CAS No.
- 487020-03-1
- Chemical Name
- N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
- Synonyms
- HI-TOPK-32;HI-TOPK-032;HI-TOPK-032 (HI TOPK 032;HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor;N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide;N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide;2-Thiophenecarboxamide, N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-
- CBNumber
- CB42695998
- Molecular Formula
- C20H11N5OS
- Formula Weight
- 369.4
- MOL File
- 487020-03-1.mol
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide Property
- Boiling point:
- 415.3±45.0 °C(Predicted)
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble3mg/mL, clear (warmed)
- pka
- 9.32±0.46(Predicted)
- form
- powder
- color
- orange-brown
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML0796
- Product name
- HI-TOPK-032
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $123
- Updated
- 2024/03/01
- Product number
- SML0796
- Product name
- HI-TOPK-032
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $482
- Updated
- 2024/03/01
- Product number
- 614849
- Product name
- TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem
- Purity
- A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC?? = 2 μM).
- Packaging
- 5MG
- Price
- $201
- Updated
- 2023/06/20
- Product number
- 19815
- Product name
- HI TOPK 032
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $34
- Updated
- 2024/03/01
- Product number
- 19815
- Product name
- HI TOPK 032
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $92
- Updated
- 2024/03/01
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide Chemical Properties,Usage,Production
Description
HI TOPK 032 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK), blocking phosphorylation of the substrate histone H2AX with an IC50 value of ~2 μM and providing complete inhibition at 5 μM. It also inhibits checkpoint kinase 1 (Chk1; IC50 = 9.6 μM). In addition, HI TOPK 032 inhibits MEK1, achieving 40% inhibition at 5 μM, but it does not alter the activities of ERK1, JNK1, or p38 MAPK at 2 μM. HI TOPK 032 decreases the growth of colon cancer and glioma initiating cells in vitro and suppresses tumor growth in vivo.
Uses
HI-TOPK-032 has been used as a PDZ binding-kinase (PBK) inhibitor.
Uses
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide is a novel TOPK inhibitor that was shown to effectively suppress colon cancer growth.
Biological Activity
HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, modulates the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
Biochem/physiol Actions
HI-TOPK-032 is a specific TOPK (T-LAK cell–originated protein kinase) inhibitor both in vitro and in vivo. HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model.
in vitro
HI-TOPK-032 strongly suppresses TOPK kinase activity but has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 also inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP.
in vivo
Treatment of mice with 1 or 10 mg/kg of HI-TOPK-032 significantly inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly induced, and phosphorylation of ERK and RSK, a direct downstream protein of ERK, is markedly inhibited in the HI-TOPK-032-treated group.
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide Preparation Products And Raw materials
Raw materials
Preparation Products
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