A ULK1 inhibitor
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XST-14

Item No. 43722

Technical Information
Formal Name
4,6-bis(1-methylethoxy)-H-indole-2-carboxylic acid, methyl ester
CAS Number
2607143-50-8
Molecular Formula
C16H21NO4
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(C1=CC2=C(N1)C=C(OC(C)C)C=C2OC(C)C)OC
InChi Code
InChI=1S/C16H21NO4/c1-9(2)20-11-6-13-12(15(7-11)21-10(3)4)8-14(17-13)16(18)19-5/h6-10,17H,1-5H3
InChi Key
ZNFMBFABCSHXPM-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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    Product Description

    XST-14 is an inhibitor of unc-51-like autophagy activating kinase 1 (ULK1; IC50 = 13.6 nM).1 It is selective for ULK1 over anaplastic lymphoma kinase 2 (ALK2), p38α MAPK, TGF-β receptor type 2 (TGFBR2), and MEK1 (IC50s = 183.8, 283.9, 809.3, and 721.8 nM, respectively) but does inhibit calcium/calmodulin-dependent kinase II (CaMKII) and ULK2 (IC50s = 66.3 and 70.9 nM, respectively). XST-14 (5 µM) induces apoptosis and autophagy and decreases invasion in HepG2 hepatocellular carcinoma cells. In vivo, XST-14, alone and in combination with sorafenib (Item Nos. 10009644 | 35612), decreases tumor volume in a HepG2 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xue, S.-T., Li, K., Gao, Y., et alThe role of the key autophagy kinase ULK1 in hepatocellular carcinoma and its validation as a treatment target. Autophagy 16(10), 1823-1837 (2020).