1404437-62-2
Chemical Structure
ML281
- CAS No.: 1404437-62-2
- Formula:C22H19N3O2S
- Molecular Weight:389.47
IUPAC Name: N-(4-isopropyl-2-(3-oxo-3,4-dihydroquinoxalin-2-yl)phenyl)thiophene-2-carboxamide
InChIKey: HWOYIOLMBQSTQS-UHFFFAOYSA-N
SMILES: O=C1NC2=CC=CC=C2N=C1C3=CC(C(C)C)=CC=C3NC(C4=CC=CS4)=O
Biological Activity: ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion[1]. ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia [4]. ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage[1][2][4]
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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ML281 | 98.04% | ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion. ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage | ||||||||||||||||||||
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References
- [1]. Sun EL, et al. Knockdown of human serine/threonine kinase 33 suppresses human small cell lung carcinoma by blocking RPS6/BAD signaling transduction. Neoplasma. 2017;64(6):869-879.
- [2]. Weïwer M, et al. A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
- [4]. Xie Y, et al. HPD degradation regulated by the TTC36-STK33-PELI1 signaling axis induces tyrosinemia and neurological damage. Nat Commun. 2019 Sep 19;10(1):4266.
