A KAT II inhibitor
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PF-04859989 (hydrochloride)

Item No. 31383

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S)-3-amino-3,4-dihydro-1-hydroxy-2(1H)-quinolinone, monohydrochloride
CAS Number
177943-33-8
Molecular Formula
C9H10N2O2 • HCl
Formula Weight
214.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 22 mg/mlWater: 22 mg/ml
SMILES
ON1C2=CC=CC=C2C[C@@H](C1=O)N.Cl
InChi Code
InChI=1S/C9H10N2O2.ClH/c10-7-5-6-3-1-2-4-8(6)11(13)9(7)12;/h1-4,7,13H,5,10H2;1H/t7-;/m0./s1
InChi Key
WZOBDOKCHIUXAY-FJXQXJEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    1 mg

    $38

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    5 mg

    $120

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    10 mg

    $218

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    25 mg

    $498

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    Product Description

    PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).1 It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kozak, R., Campbell, B.M., Strick, C.A., et al. Reduction of brain kynurenic acid improves cognitive function. J. Neurosci. 34(32), 10592-10602 (2014).

    2. Yoshida, T., Yamasaki, S., Kaneko, O., et al. A covalent small molecule inhibitor of glutamate-oxaloacetate transaminase 1 impairs pancreatic cancer growth. Biochem. Biophys. Res. Commun. 522(3), 633-638 (2020).

    Product Citations

    Kremer, D.M., Nelson, B.S., Lin, L., et al. GOT1 inhibition primes pancreatic cancer for ferroptosis through the autophagic release of labile iron. bioRxiv (2020).