1. Apoptosis
  2. MDM-2/p53
  3. SCH529074

SCH529074 

Cat. No.: HY-110088
Handling Instructions

SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).

For research use only. We do not sell to patients.

SCH529074 Chemical Structure

SCH529074 Chemical Structure

CAS No. : 922150-11-6

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Description

SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC)[1][2].

IC50 & Target

Ki: 1-2 μM (p53 DBD)[2]

In Vitro

SCH529074 (2-4 µM; 24 hours) causes significant reduction in cell viability, it causes a significant decreasing to 20-25% in p53 mutant cells (H157, H1975 and H322) and to 68% in the p53 WT cell line A549 at 4 µM[1].
SCH 529074 (2 and 4 µM) induces NSCLC cells (H157, A549, HCT116 and HCT116 p53-/-) arrested at the G0/G1 phase (59%; 72%; 66%; and 57%) compared with the control cells following low concentration (2 µM) of treatment[1].
SCH 529074 (2-4 µM; 24 hours) induces the early and late apoptotic rates at 2 µM in H1975 cells. In H157 cells, SCH 529074 treatment induces early and late apoptosis. Similarly, in A549 cells, 2 and 4 µM of SCH 529074 significantly increased early and late apoptosis. In line with that, in colon cancer cells, in HCT116 cells, 4 µM of SCH 529074 causes a significant induction of early and late apoptosis, and 4 µM of SCH 529074 significantly induces early apoptosis in HCT116 p53-/- cells[1].
SCH 529074 (2-6 µM; 24 hours) increases the protein levels of PUMA and p21 revealed to 4 or 6 µM in the cancer cell lines regardless of their p53 status[1].

Cell Viability Assay[1]

Cell Line: p53 mutant cells (H157, H1975 and H322) and p53 WT cell line A549
Concentration: 2 µM; 4 µM
Incubation Time: 24 hours
Result: Inhibited cancer WT and mutant cell viability.

Cell Cycle Analysis[1]

Cell Line: H1975, H157, A549, HCT116, HCT116 p53-/- cells
Concentration: 2 µM, 4 µM, 6 µM
Incubation Time: 24 hours
Result: Induced apoptosis in all assessed NSCLC cell lines irrespective of their p53 mutational status.

Western Blot Analysis[1]

Cell Line: H1975, H322, H157, A549, HCT116, HCT116 p53-/-
Concentration: 2 µM, 4 µM, 6 µM
Incubation Time: 24 hours
Result: Increased PUMA and p21 protein expression.
In Vivo

SCH529074 (oral administration; 30 or 50 mg/kg; twice daily; 4 weeks; started on day 3 until day 31) causes 79 and 43% reduction of tumor growth at 50 and 30 mg/kg doses, respectively. the degree of tumor inhibition correlates with the plasma exposure of the compound (0.26–0.55 μm at 30 mg/kg and 0.39-0.79 μm at 50 mg/kg, 2-12 h post final dosing) in human DLD-1 colorectal cancer xenograft[2].

Animal Model: Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells[2]
Dosage: 30 or 50 mg/kg
Administration: Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result: Inhibited tumor growth
Molecular Weight

563.56

Formula

C₃₁H₃₆Cl₂N₆

CAS No.

922150-11-6

SMILES

CN(C)CCCNC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vivo:
  • 1.

    It is in 20% hydroxylpropyl-β-cyclodextran as well as vehicle[2]

References
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Keywords:

SCH529074SCH 529074SCH-529074MDM-2/p53NSCLCHCT116WiDrDLD-1KLEH322MCF7SJSAWS-1MB-468cellsInhibitorinhibitorinhibit

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