N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide

ChemicalBook > CAS DataBase List > N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide

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

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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

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Safety

Hazard Codes: Xn
Risk Statements: 22
WGK Germany: 3
HS Code: 2922500090

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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..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0796
Product name: HI-TOPK-032
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $123
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0796
Product name: HI-TOPK-032
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $482
Updated: 2024/03/01

Sigma-Aldrich

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

Cayman Chemical

Product number: 19815
Product name: HI TOPK 032
Purity: ≥95%
Packaging: 1mg
Price: $34
Updated: 2024/03/01

Cayman Chemical

Product number: 19815
Product name: HI TOPK 032
Purity: ≥95%
Packaging: 5mg
Price: $92
Updated: 2024/03/01

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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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487020-03-1, N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMideRelated Search:

N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide

HI-TOPK-032

HI-TOPK-32

N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide

HI-TOPK-032 (HI TOPK 032

2-Thiophenecarboxamide, N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-

HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor

487020-03-1

C20H11N5OS

Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds