A dual inhibitor of POLA1 and HDAC11
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GEM144

Item No. 44647

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-3-[4′-[2-(hydroxyamino)-1-methyl-2-oxoethoxy]-3′-tricyclo[3.3.1.13,7]dec-1-yl[1,1′-biphenyl]-4-yl]-2-propenoic acid
CAS Number
2487526-28-1
Molecular Formula
C28H31NO5
Formula Weight
461.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C(NO)=O)OC1=C(C=C(C(C=C2)=CC=C2/C=C/C(O)=O)C=C1)C3(C[C@H](C4)C5)CC5CC4C3
InChi Code
InChI=1S/C28H31NO5/c1-17(27(32)29-33)34-25-8-7-23(22-5-2-18(3-6-22)4-9-26(30)31)13-24(25)28-14-19-10-20(15-28)12-21(11-19)16-28/h2-9,13,17,19-21,33H,10-12,14-16H2,1H3,(H,29,32)(H,30,31)/b9-4+/t17?,19-,20?,21?,28?
InChi Key
PIJPEZHKJKJZHS-PMWLYXLASA-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

    $49

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    5 mg

    $159

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    10 mg

    $270

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    25 mg

    $551

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    Cayman Chemical
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    Product Description

    GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11).1 It inhibits the primer extension activity of POLA1 in a cell-free assay when used at concentrations ranging from 10 to 50 µM and increases acetylation of α-tubulin at lysine 40 in H460 lung cancer cells at 0.4 µM. It inhibits proliferation in a panel of cancer cell lines, including three malignant melanoma (IC50s = 0.73-1.4 µM), six hematological (IC50s = 0.16-3.2 µM), one breast cancer (IC50 = 0.77 µM), and one glioma cell line (IC50 = 1 µM). GEM144 (50 mg/kg) reduces tumor growth in an H460 mouse xenograft model and an MM487 orthotopic, malignant pleural mesothelioma xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dallavalle, S., Musso, L., Cincinelli, R., et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur. J. Med. Chem. 228, 113971 (2022).