A Cdk2 and Cdk5 inhibitor
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GW 8510

Item No. 43576

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(6,7-dihydro-7-oxo-8H-pyrrolo[2,3-g]benzothiazol-8-ylidene)methyl]amino]-N-2-pyridinyl-benzenesulfonamide
CAS Number
222036-17-1
Molecular Formula
C21H15N5O3S2
Formula Weight
449.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=S(NC1=NC=CC=C1)(C2=CC=C(NC=C(C3=C(N4)C=CC5=C3SC=N5)C4=O)C=C2)=O
InChi Code
InChI=1S/C21H15N5O3S2/c27-21-15(19-16(25-21)8-9-17-20(19)30-12-24-17)11-23-13-4-6-14(7-5-13)31(28,29)26-18-3-1-2-10-22-18/h1-12,23H,(H,22,26)(H,25,27)
InChi Key
GCYXEGSPUDSZJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $116

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    10 mg

    $208

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    25 mg

    $434

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    50 mg

    $693

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    Product Description

    GW 8510 is an inhibitor of cyclin-dependent kinase 2 (Cdk2) and Cdk5 (IC50s = 3, 3, and 7 nM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk5/p25 complexes, respectively).1 It is selective for Cdk2 and Cdk5 over Cdk1/cyclin B, Cdk4/cyclin D, Cdk7/cyclin H, and Cdk9/cyclin T (IC50s = 49, 139, 317, and 543 nM, respectively). It also decreases ribonucleoside-diphosphate reductase subunit M2 (RRM2) levels and induces autophagy in HCT116 colon cancer cells when used at a concentration of 4 µM.2 GW 8510 (1-500 nM) protects against MPP+-induced cytotoxicity in primary human neural progenitor cells derived from induced pluripotent stem cells (iPSCs) in an in vitro model of Parkinson’s disease.3 In vivo, GW 8510 (2 mg/kg) increases grip strength and gastrocnemius and soleus muscle-to-body weight ratios in a mouse model of muscle atrophy induced by sciatic nerve denervation.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jorda, R., Hendrychová, D., Voller, J., et al. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J. Med. Chem. 61(20), 9105-9120 (2018).

    2. Hsieh, Y.-Y., Chou, C.-J., Lo, H.-L., et al. Repositioning of a cyclin-dependent kinase inhibitor GW8510 as a ribonucleotide reductase M2 inhibitor to treat human colorectal cancer. Cell Death Discov. 2, 16027 (2016).

    3. Wimalasena, N.K., Le, V.Q., Wimalasena, K., et al. Gene expression-based screen for Parkinson’s disease identifies GW8510 as a neuroprotective agent. ACS Chem. Neurosci. 7(7), 857-863 (2016).

    4. Chen, Y., Liu, Z., Liu, C., et al. GW8510 alleviates muscle atrophy and skeletal muscle dysfunction in mice through AMPK/PGC1α signaling. Int. J. Mol. Med. 56(3), 128 (2025).