A HAT1 inhibitor
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JG-2016

Item No. 41876

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-chloro-8-ethyl-10-[2-(2-methylpropoxy)ethyl]-benzo[g]pteridine-2,4(3H,10H)-dione
CAS Number
2887480-87-5
Molecular Formula
C18H21ClN4O3
Formula Weight
376.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1N=C2C(C(N1)=O)=NC3=C(N2CCOCC(C)C)C=C(CC)C(Cl)=C3
InChi Code
InChI=1S/C18H21ClN4O3/c1-4-11-7-14-13(8-12(11)19)20-15-16(21-18(25)22-17(15)24)23(14)5-6-26-9-10(2)3/h7-8,10H,4-6,9H2,1-3H3,(H,22,24,25)
InChi Key
IOHJEWFKBRNJIO-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

    $83

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    5 mg

    $351

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    10 mg

    $537

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    25 mg

    $1,032

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    Cayman Chemical
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    Product Description

    JG-2016 is an inhibitor of histone acetyltransferase 1 (HAT1; IC50 = 14.8 µM).1 It is selective for HAT1 over lysine acetyltransferase 2A (KAT2A/GCN5) and p300/CBP-associated factor (PCAF), for which it has no activity, KAT5, KAT6B, and KAT7 (IC50s = >100, >100, and 84.82 µM, respectively), CREB-binding protein (CBP), and p300 (IC50s = 90.41 and 74.25 µM, respectively). JG-2016 (20 µM) reduces acetylation of histone H4 lysine 5 (H4K5) and H4K12 in hTert-HME1 mammary epithelial cells. It reduces the growth of HCC1806 triple-negative breast cancer and A549 lung cancer cells (EC50s = 10.4 and 1.9 µM, respectively). JG-2016 reduces intratumoral H4K12 acetylation in an A549 mouse xenograft model in a dose-dependent manner. It also reduces tumor growth in an A549 mouse xenograft model when administered at doses of 50 and 100 mg/kg once every three days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gaddameedi, J.D., Chou, T., Geller, B.S., et al. An acetyl-click screening platform identifies small-molecule inhibitors of histone acetyltransferase 1 (HAT1). J. Med. Chem. 66(8), 5774-5801 (2023).