A PARP14 inhibitor
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RBN-012759

Item No. 36137

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-(cyclopropylmethoxy)-5-fluoro-2-[[(trans-4-hydroxycyclohexyl)thio]methyl]-4(3H)-quinazolinone
CAS Number
2360851-29-0
Molecular Formula
C19H23FN2O3S
Formula Weight
378.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
243 nm
SMILES
FC1=C2C(NC(CS[C@@H]3CC[C@H](CC3)O)=NC2=O)=CC(OCC4CC4)=C1
InChi Code
InChI=1S/C19H23FN2O3S/c20-15-7-13(25-9-11-1-2-11)8-16-18(15)19(24)22-17(21-16)10-26-14-5-3-12(23)4-6-14/h7-8,11-12,14,23H,1-6,9-10H2,(H,21,22,24)/t12-,14-
InChi Key
NKZDEFKPZSLQRF-MQMHXKEQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $76

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    5 mg

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    10 mg

    $456

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    25 mg

    $950

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    Cayman Chemical
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    Product Description

    RBN-012759 is an inhibitor of poly(ADP-ribose) polymerase 14 (PARP14; IC50 = 0.003 µM).1 It is selective for PARP14 over PARP1-4, -5a, -5b, -6-12, -15, and -16 (IC50s = 1->100 µM). RBN-012759 (10 µM) inhibits IFN-γ-induced PARP14 auto-MARylation in CFPAC-1 cells. It inhibits IL-4-induced protumor M2-like macrophage polarization in isolated human primary macrophages. RBN-012759 (1 µM) also induces expression of the genes encoding the pro-inflammatory chemokines chemokine (C-C motif) ligand 13 (CCL13), CCL19, and chemokine (C-X-C motif) ligand 11 (CXCL11) in human kidney cancer tumor explants.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schenkel, L.B., Molina, J.R., Swinger, K.K., et al. A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants. Cell Chem. Biol. 28(8), 1158-1168.e1113 (2021).