N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
![N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide Structure](CAS/GIF/487020-03-1.gif)
- CAS No.
- 487020-03-1
- Chemical Name:
- N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
- Synonyms
- HI-TOPK-032;HI-TOPK-32;HI-TOPK-032 (HI TOPK 032;HI-TOPK-032, 10 mM in DMSO;TOPK/PBK Inhibitor, 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;N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide;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
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| HI-TOPK-032 ≥98% (HPLC) | SML0796 | 5mg | $115 |
| HI-TOPK-032 ≥98% (HPLC) | SML0796 | 25mg | $453 |
| 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). | 614849 | 5MG | $181 |
| HI TOPK 032 ≥95% | 19815 | 1mg | $38 |
| HI TOPK 032 ≥95% | 19815 | 5mg | $102 |
| More product size | |||
| 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) |
| form | powder |
| pka | 9.32±0.46(Predicted) |
| color | orange-brown |
| 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) |
| InChIKey | BCSBXWKRZUPFHW-UHFFFAOYSA-N |
| SMILES | [s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2 |
| FDA UNII | VH977A8H53 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  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 | |||||||||
| Storage Class | 11 - Combustible Solids | |||||||||
| NFPA 704 |
|
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide price More Price(26)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0796 | HI-TOPK-032 ≥98% (HPLC) | 487020-03-1 | 5mg | $115 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML0796 | HI-TOPK-032 ≥98% (HPLC) | 487020-03-1 | 25mg | $453 | 2026-04-30 | 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 | $181 | 2025-07-31 | Buy |
| Cayman Chemical | 19815 | HI TOPK 032 ≥95% | 487020-03-1 | 1mg | $38 | 2026-04-30 | Buy |
| Cayman Chemical | 19815 | HI TOPK 032 ≥95% | 487020-03-1 | 5mg | $102 | 2026-04-30 | 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.
References
[1] DONG JOON KIM. Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth.[J]. Cancer research, 2012: 3060-3068. DOI: 10.1158/0008-5472.can-11-3851
[2] YAN LI. Discovery of Novel Checkpoint Kinase 1 Inhibitors by Virtual Screening Based on Multiple Crystal Structures[J]. Journal of Chemical Information and Modeling , 2011, 51 11: 2904-2914. DOI: 10.1021/ci200257b
[3] MRINAL JOEL. Targeting PBK/TOPK decreases growth and survival of glioma initiating cells in vitro and attenuates tumor growth in vivo.[J]. Molecular Cancer, 2015: 121. DOI: 10.1186/s12943-015-0398-x
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +86-13203830695 | laboratory@coreychem.com | China | 30203 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +86-18621343501 | product@acmec-e.com | China | 33301 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 54746 | 58 | |
| Shaanxi Dideu New Materials Co. Ltd | 18192503167 | 1036@dideu.com | China | 13339 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131885 | 58 |
| J & K SCIENTIFIC LTD. | 18210857532 18210857532 | jkinfo@jkchemical.com | China | 96815 | 76 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD | 13816107857 | sales@fortunechem-sh.com | China | 981 | 58 |
| Nanjing Dulai Biotechnology Co., Ltd. | 025-84699383-8003;025-846993838003-8003 18013301590 | njduly@126.com | China | 3293 | 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 | |
|---|---|---|---|---|---|---|---|---|
 |
2026-07-14 | HI-TOPK-032
487020-03-1
|
1KG | 98% | 20Tons | Shaanxi Dideu New Materials Co. Ltd | ||
 |
2026-04-21 | HI-TOPK-032
487020-03-1
|
$63.00-198.00 | 98.69% | 10g | TargetMol Chemicals Inc. |
-
- HI-TOPK-032
487020-03-1
- 98%
- Shaanxi Dideu New Materials Co. Ltd
-
- HI-TOPK-032
487020-03-1
- $63.00-198.00
- 98.69%
- TargetMol Chemicals Inc.
