An inhibitor of STK33
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ML-281

Item No. 20116

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(3,4-dihydro-3-oxo-2-quinoxalinyl)-4-(1-methylethyl)phenyl]-2-thiophenecarboxamide
CAS Number
1404437-62-2
Molecular Formula
C22H19N3O2S
Formula Weight
389.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 20 mg/ml
λmax
284 nm
SMILES
O=C1NC2=CC=CC=C2N=C1C3=C(C=CC(C(C)C)=C3)NC(C4=CC=CS4)=O
InChi Code
InChI=1S/C22H19N3O2S/c1-13(2)14-9-10-16(24-21(26)19-8-5-11-28-19)15(12-14)20-22(27)25-18-7-4-3-6-17(18)23-20/h3-13H,1-2H3,(H,24,26)(H,25,27)
InChi Key
HWOYIOLMBQSTQS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $236

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    25 mg

    $544

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    Product Description

    ML-281 is an inhibitor of the serine/threonine kinase STK33 (IC50 = 14 nM for purified, recombinant STK33), a kinase whose downregulation is toxic to KRAS-dependent cancer cell lines.1 It has 700- and 550-fold selectivity for STK33 over PKA and Aurora B kinase, respectively. It is also selective over 81 other kinases in a panel at a concentration of 1 µM, but does inhibit the activity of Fms-like tyrosine kinase (FLT3) and vascular endothelial growth factor receptor 2 (VEGFR2/KDR) by greater than 25%. ML-281 does not decrease viability of KRAS-dependent or KRAS-independent cell lines.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Weïwer, M., Spoonamore, J., Wei, J., et al. A potent and selective quinoxalinone-based STK33 inhibitor does not show synthetic lethality in KRAS-dependent cells. ACS Med. Chem. Lett. 3(12), 1034-1038 (2012).