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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

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;HI-TOPK-032, 10 mM in DMSO;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
Molecular Weight:
369.4
MDL Number:
MFCD03286313
MOL File:
487020-03-1.mol
MSDS File:
SDS
Last updated:2025-01-27 09:38:02

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

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
FDA UNII VH977A8H53
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501
Hazard Codes  Xn
Risk Statements  22
WGK Germany  3
HS Code  2922500090
NFPA 704
0
2 0

N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide price More Price(20)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0796 HI-TOPK-032 ≥98% (HPLC) 487020-03-1 5mg $123 2024-03-01 Buy
Sigma-Aldrich SML0796 HI-TOPK-032 ≥98% (HPLC) 487020-03-1 25mg $482 2024-03-01 Buy
Sigma-Aldrich 614849 TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC?? = 2 μM). 487020-03-1 5MG $201 2023-06-20 Buy
Cayman Chemical 19815 HI TOPK 032 ≥95% 487020-03-1 1mg $34 2024-03-01 Buy
Cayman Chemical 19815 HI TOPK 032 ≥95% 487020-03-1 5mg $92 2024-03-01 Buy
Product number Packaging Price Buy
SML0796 5mg $123 Buy
SML0796 25mg $482 Buy
614849 5MG $201 Buy
19815 1mg $34 Buy
19815 5mg $92 Buy

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

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.

Uses

HI-TOPK-032 has been used as a PDZ binding-kinase (PBK) inhibitor.

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

Global( 68)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32161 58
Career Henan Chemica Co 		+86-0371-86658258 +8613203830695 laboratory@coreychem.com China 30233 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
Shanghai Acmec Biochemical Technology Co., Ltd. 		+86-18621343501; +undefined18621343501 product@acmec-e.com China 33338 58
Aladdin Scientific 		tp@aladdinsci.com United States 57505 58
SHANGHAI KEAN TECHNOLOGY CO., LTD. 		+8613817748580 cooperation@kean-chem.com China 40066 58
Amadis Chemical Company Limited 		571-89925085 sales@amadischem.com China 131957 58
J & K SCIENTIFIC LTD. 010-82848833 400-666-7788 jkinfo@jkchemical.com China 96815 76
Shanghai TaoSu Biochemical Technology Co., Ltd. 021-33632979 info@tsbiochem.com China 8065 58
Shanghai XingMo Biotechnology Co., Ltd. +86 13524779951; 13524779951 2075692521@qq.com China 310 55

View Lastest Price from N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
HI-TOPK-032 pictures 2024-11-19 HI-TOPK-032
487020-03-1
 US $39.00-94.00 / mg 98.52% 10g TargetMol Chemicals Inc.
  • HI-TOPK-032 pictures
  • HI-TOPK-032
    487020-03-1
  • US $39.00-94.00 / mg
  • 98.52%
  • TargetMol Chemicals Inc.

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

N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide HI-TOPK-032 HI-TOPK-32 2-Thiophenecarboxamide, N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)- HI-TOPK-032 (HI TOPK 032 N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor HI-TOPK-032, 10 mM in DMSO 487020-03-1 C20H11N5OS Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds