2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. OAT-4828

OAT-4828 is an orally active ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 32 nM. OAT-4828 induces antileukemic activity in B-cell-derived non-Hodgkin's lymphoma models via inhibition of USP7. OAT-4828 is applicable to research related to chronic lymphocytic leukemia.

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OAT-4828

OAT-4828 Chemical Structure

CAS No. : 2947497-65-4

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OAT-4828 Related Antibodies

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USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

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Description

OAT-4828 is an orally active ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 32 nM. OAT-4828 induces antileukemic activity in B-cell-derived non-Hodgkin's lymphoma models via inhibition of USP7. OAT-4828 is applicable to research related to chronic lymphocytic leukemia[1].

IC50 & Target[1]

USP7

32 nM (IC50)

In Vitro

OAT-4828 inhibits hERG potassium channels with an IC50 of 36 μM in a binding assay and 7.4 μM in a QPatch assay[1].

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

OAT-4828 Related Antibodies
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-inf T1/2 Bioavailability CL Vss
Mice[1] 3 mg/kg i.v. / / 1324 ng·h/mL 0.45 h / 37.8 mL/min/kg 0.9 L/kg
Mice[1] 10 mg/kg p.o. 0.5 h 172 ng/mL 516 ng·h/mL 0.92 h 12 % / /
Rat[1] 3 mg/kg i.v. / / 792 ng·h/mL 5.0 h / 64.1 mL/min/kg 12.7 L/kg
Rat[1] 10 mg/kg p.o. 2 h 53.6 ng/mL 352 ng·h/mL 5.0 h 13 % / /
Rat[1] 50 mg/kg p.o. 4 h 1158 ng/mL 5262 ng·h/mL 2.9 h / / /
Dog[1] 3 mg/kg i.v. / / 979 ng·h/mL 4.4 h / 51.7 mL/min/kg 12.7 L/kg
Dog[1] 10 mg/kg p.o. 2 h 526 ng/mL 3564 ng·h/mL 4.5 h 109 % / /
Dog[1] 50 mg/kg p.o. 2 h 3367 ng/mL 26615 ng·h/mL 6.0 h / / /
In Vivo

Administration of OAT-4828 (50 mg/kg; p.o.; twice daily for 21 days) exerts significant antileukemic activity, reducing blood leukemia cell burden by up to 74% and decreasing spleen weight in a mouse model of chronic lymphocytic leukemia, with favorable tolerance[1].

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

Animal Model: C57BL6/J (female, 6−12 weeks old, adoptive transfer of 5×106 leukemic CD5+CD19+ TCL1 cells via tail vein injection)[1]
Dosage: 50 mg/kg
Administration: p.o.; twice daily for 21 days
Result: Reduced the percentage of leukemic CD5+CD19+ cells in blood by up to 74% on day 17 compared to vehicle control.
Significantly reduced spleen weight relative to vehicle control on day 21.
Caused no significant body weight loss.
Molecular Weight

571.61

Formula

C28H28F3N5O3S
CAS No.
SMILES

CN[C@H]1CCN(C1)C(C2=C(C=C(N=C2C3=C4SC(CN5C(C6C(C6(C)C)C5=O)=O)=CC4=NC=C3)C(F)(F)F)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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OAT-4828 Related Classifications

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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:

OAT-48282947497-65-4OAT4828OAT 4828DeubiquitinaseDUBsubiquitin-specific protease 7B-cell derived chronic lymphocytic leukemiahERG potassium channelsB-cell derived non-Hodgkin lymphomaCYP450 isoformsmice5-HT2A receptorUSP7Caco-2Inhibitorinhibitorinhibit

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