2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. USP1-IN-9

USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer.

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USP1-IN-9 Chemical Structure

USP1-IN-9 Chemical Structure

CAS No. : 2925548-22-5

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USP1-IN-9 Related Antibodies

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：结束 是行
Pharmacokinetic parameters of USP1-IN-9 in Mice[1]

药代动力学分析[1]
Description

USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer[1].
IC50 & Target[1]

USP-1

8.8 nM (IC50)

In Vitro

USP1-IN-9 (20, 100, 500 nM, 24 h) elevates the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner. USP1-IN-9 demonstrates an increase in Ub-PCNA even at concentrations as low as 20 nM in nonsmall cell lung cancer (NSCLC) cells[1].
USP1-IN-9 (0.5 μM, 7 days) exhibites a substantial inhibition of the colony forming capacity of NSCLC cells[1].
USP1-IN-9 (1 nM, 24 h) alone results in a minor cell cycle arrest in olaparib-resistant breast cancer cells, whereas the combination of olaparib (HY-10162) and USP1-IN-9 can induce cell cycle arrest[1].
USP1-IN-9 (100 nM, 7 days) combined with olaparib can potentiate breast cancer cells to olaparib killing[1].

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

USP1-IN-9 Related Antibodies

Western Blot Analysis[1]

Cell Line: NSCLC cells
Concentration: 20, 100, 500 nM
Incubation Time: 24 h
Result: Elevated the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner in NSCLC cells.

Cell Viability Assay[1]

Cell Line: NSCLC cells
Concentration: 0.5 nM
Incubation Time: 7 days
Result: Exhibited a substantial inhibition of the colony forming capacity of breast cancer cells compared to the untreated control.

Cell Cycle Analysis[1]

Cell Line: Breast cancer cells and olaparib-resistant breast cancer cells
Concentration: 1 nM
Incubation Time: 24 h
Result: Resulted in a minor increase in cells within the S phase, whereas the combination of olaparib and USP1-IN-9 led to an accumulation of cells within the S phase and G2/M phase.

Cell Viability Assay[1]

Cell Line: Olaparib-resistant breast cancer cells
Concentration: 100 nM
Incubation Time: 7 days
Result: Alone exhibited a reduction of 30% and did not demonstrate significant cell killing. The inhibition rate of colony formation was further elevated to 50 % combined with USP1-IN-9 and olaparib(100 nM).
In Vivo

USP1-IN-9 (10 mg/kg, i.g.) is absorbed rapidly and shows good metabolic stability on male ICR mice[1].
合并列 符号

： 代表后面的三列被合并 是列
Parameters Dose (mg/kg,po) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) T1/2 (h)
USP1-IN-9 10 0.25 4780 ± 2090 35,800 ± 13,500 7.61 ± 4.67

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

Animal Model: male ICR mice
Dosage: 10 mg/kg
Administration: i.g., a single dose
Result: Was absorbed rapidly and showed good metabolic stability with a long half-life of 7.61 h on male ICR mice.
Molecular Weight

561.56

Formula

C29H26F3N7O2

CAS No. SMILES

O=C1C=CC2=CN=C(C3=C(C4CC4)N=CN=C3OC)N=C2N1CC5=CC=C(C6=NC(C(F)(F)F)=CN6C(C)C)C=C5

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation References
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USP1-IN-9 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:

USP1-IN-92925548-22-5DeubiquitinaseDUBsantiproliferation effectolaparib-resistant breast cancer cellsmale ICR miceInhibitorinhibitorinhibit

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