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  4. UPF-648

UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.

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UPF-648 Chemical Structure

UPF-648 Chemical Structure

CAS No. : 213400-34-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 48 In-stock
Solid
2 mg USD 34 In-stock
5 mg USD 69 In-stock
10 mg USD 110 In-stock
25 mg USD 230 In-stock
50 mg USD 368 In-stock
100 mg USD 588 In-stock
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Based on 1 publication(s) in Google Scholar

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UPF-648 Related Antibodies

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Description

UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.

In Vitro

BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity[1].
UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

UPF-648 Related Antibodies
In Vivo

Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA[1].
Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels[2].
UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

259.09

Formula

C11H8Cl2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1[C@@H](C(C2=CC=C(Cl)C(Cl)=C2)=O)C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

Ethanol : ≥ 50 mg/mL (192.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8597 mL 19.2983 mL 38.5966 mL
5 mM 0.7719 mL 3.8597 mL 7.7193 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 3.8597 mL 19.2983 mL 38.5966 mL 96.4916 mL
5 mM 0.7719 mL 3.8597 mL 7.7193 mL 19.2983 mL
10 mM 0.3860 mL 1.9298 mL 3.8597 mL 9.6492 mL
15 mM 0.2573 mL 1.2866 mL 2.5731 mL 6.4328 mL
20 mM 0.1930 mL 0.9649 mL 1.9298 mL 4.8246 mL
25 mM 0.1544 mL 0.7719 mL 1.5439 mL 3.8597 mL
30 mM 0.1287 mL 0.6433 mL 1.2866 mL 3.2164 mL
40 mM 0.0965 mL 0.4825 mL 0.9649 mL 2.4123 mL
50 mM 0.0772 mL 0.3860 mL 0.7719 mL 1.9298 mL
60 mM 0.0643 mL 0.3216 mL 0.6433 mL 1.6082 mL
80 mM 0.0482 mL 0.2412 mL 0.4825 mL 1.2061 mL
100 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9649 mL
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UPF-648 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UPF-648213400-34-1UPF648UPF 648OthersInhibitorinhibitorinhibit

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