A PROTAC that drives hexokinase 2 degradation
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C-02

Item No. 39384

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(2,4-dichlorophenyl)methyl]-N-[4-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]butyl]-1H-indazole-3-carboxamide
CAS Number
3033812-84-6
Molecular Formula
C32H28Cl2N6O5
Formula Weight
647.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: SolubleMethanol: Soluble
SMILES
O=C(N(C1C(NC(CC1)=O)=O)C2=O)C3=C2C=CC=C3NCCCCNC(C4=NN(CC5=C(Cl)C=C(Cl)C=C5)C6=C4C=CC=C6)=O
InChi Code
InChI=1S/C32H28Cl2N6O5/c33-19-11-10-18(22(34)16-19)17-39-24-9-2-1-6-20(24)28(38-39)30(43)36-15-4-3-14-35-23-8-5-7-21-27(23)32(45)40(31(21)44)25-12-13-26(41)37-29(25)42/h1-2,5-11,16,25,35H,3-4,12-15,17H2,(H,36,43)(H,37,41,42)
InChi Key
OFEUWOIETWIJID-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

    $323

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    Cayman Chemical
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    Product Description

    C-02 is a proteolysis-targeting chimera (PROTAC) composed of the hexokinase inhibitor lonidamine (Item No. 14640) linked to the cereblon ligand thalidomide (Item No. 14610).1 It induces degradation of hexokinase 2 in 786-O and PANC-1 cells when used at a concentration of 20 µM. C-02 is cytotoxic to 786-O, 4T1, PANC-1, HGC-27, and MCF-7 cancer cells (IC50s = 34.07, 5.08, 31.53, 6.11, and 21.65 µM, respectively). It reduces the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, indicating inhibition of glycolysis and mitochondrial damage, respectively, when used at a concentration of 20 µM. In vivo, C-02 (50 mg/kg) reduces tumor volume and induces intratumoral cytokine accumulation and pyroptosis in a 4T1 murine mammary carcinoma model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sang, R., Fan, R., Deng, A., et al. Degradation of hexokinase 2 blocks glycolysis and induces GSDME-dependent pyroptosis to amplify immunogenic cell death for breast cancer therapy. J. Med. Chem. 66(13), 8464-8483 (2023).