An inhibitor of type I PRMTs
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GSK3368715 (hydrochloride)

Item No. 34886

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-1,2-ethanediamine, monohydrochloride
CAS Number
2227587-25-7
Molecular Formula
C20H38N4O2 • HCl
Formula Weight
403.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 40 mg/ml
SMILES
CN(CCNC)CC1=CNN=C1C2CCC(COCC)(COCC)CC2.Cl
InChi Code
InChI=1S/C20H38N4O2.ClH/c1-5-25-15-20(16-26-6-2)9-7-17(8-10-20)19-18(13-22-23-19)14-24(4)12-11-21-3;/h13,17,21H,5-12,14-16H2,1-4H3,(H,22,23);1H
InChi Key
WRVJUOWIQSTJPE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $85

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    5 mg

    $374

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    10 mg

    $663

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    Cayman Chemical
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    Product Description

    GSK3368715 is an inhibitor of type I protein arginine methyltransferases (PRMTs; IC50s = 3.1, 162, 38, 4.7, and 39 nM for PRMT1, 3, 4, 6, and 8, respectively).1 It is selective for type I PRMTs over PRMT5, 7, and 9 (IC50s = >20,408, >40,000, and >15,000 nM, respectively), as well as 20 additional methyltransferases and a panel of ion channels, receptors, and transporters at 10 µM. GSK3368715 (5 µM) inhibits the growth of patient-derived diffuse large B cell lymphoma (DLBCL) cells. In vivo, GSK3368715 (9.375-150 mg/kg) reduces tumor volume in Toledo DLBCL and BxPC-3 pancreatic adenosarcoma mouse xenograft models. It also reduces tumor growth in ACHN renal carcinoma and MDA-MB-468 breast cancer mouse xenograft models and a pancreatic adenocarcinoma patient-derived xenograft (PDX) mouse model when administered at doses of 150 and 300 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fedoriw, A., Rajapurkar, S.R., O'Brien, S., et al. Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss. Cancer Cell 36(1), 100-114.e125 (2019).