An inhibitor of TG2
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GK921

Item No. 34359

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]-pyrido[2,3-b]pyrazine
CAS Number
1025015-40-0
Molecular Formula
C21H20N4O
Formula Weight
344.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
226, 362, 378 nm
SMILES
C1(C#CC2=CC=CC=C2)=NC3=C(N=C1OCCN4CCCC4)C=CC=N3
InChi Code
InChI=1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2
InChi Key
MNYJJHBAEYKXEG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $75

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    5 mg

    $333

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    10 mg

    $516

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    25 mg

    $827

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    Cayman Chemical
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    Product Description

    GK921 is an inhibitor of transglutaminase 2 (TG2; IC50 = 7.71 µM).1 It is cytotoxic against a panel of eight renal cell carcinoma (RCC) cell lines (mean GI50 = 0.905 µM). GK921 (8 mg/kg) suppresses tumor growth in ACHN and Caki-1 RCC mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ku, B.M., Kim, S.-J., Kim, N., et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J. Cancer Res. Clin. Oncol. 140(5), 757-767 (2014).