An inhibitor of KLK6
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DKFZ-251

Item No. 46719

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methyl-1H-indole-3-acetic acid, 2-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)amino]-2-oxoethyl ester
CAS Number
2222059-70-1
Molecular Formula
C24H24N4O3
Formula Weight
416.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CC1=C(CC(OCC(NC2=C(N(N=C2C)C3=CC=CC=C3)C)=O)=O)C4=C(C=CC=C4)N1
InChi Code
InChI=1S/C24H24N4O3/c1-15-20(19-11-7-8-12-21(19)25-15)13-23(30)31-14-22(29)26-24-16(2)27-28(17(24)3)18-9-5-4-6-10-18/h4-12,25H,13-14H2,1-3H3,(H,26,29)
InChi Key
OWHVQGGLXPNNBI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $100

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    10 mg

    $190

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    25 mg

    $350

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    50 mg

    $550

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    Cayman Chemical
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    Product Description

    DKFZ-251 is an inhibitor of kallikrein-6 (KLK6), also known as neurosin or protease M (IC50 = 0.13 µM).1 It is selective for KLK6 over KLK4, -5, -7, -8, 13, -14, and trypsin (IC50s = >200, 1.1, 73, >10, >10, 10.3, and 21 µM, respectively). DKFZ-251 increases the proliferation of FaDu head and neck squamous cell carcinoma cells and induces the epithelial-to-mesenchymal transition (EMT) in the same cells. DKFZ-251 increases the area of myelin basic protein-positive (MBP+) and myelin proteolipid protein-positive (PLP+) oligodendrocytes in primary mouse oligodendrocytes progenitor cell (OPC) cultures at 500 nM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. De Vita, E., Schüler, P., Lovell, S., et al. Depsipeptides featuring a neutral P1 are potent inhibitors of kallikrein-related peptidase 6 with on-target cellular activity. J. Med. Chem. 61(19), 8859-8874 (2018).

    2. Yoon, H., Triplet, E.M., Simon, W.L., et al. Blocking Kallikrein 6 promotes developmental myelination. Glia 70(3), 430-450 (2022).