2. Apoptosis
  3. MDM-2/p53
  4. Siremadlin succinate

Siremadlin succinate  (Synonyms: NVP-HDM201 succinate; HDM201 succinate)

Cat. No.: HY-18658B
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Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma.

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

Siremadlin succinate

Siremadlin succinate Chemical Structure

CAS No. : 1638193-48-2

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Siremadlin succinate Related Antibodies

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Description

Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma[1].

In Vitro

Siremadlin (NVP-HDM201) succinate (72 h) had its growth-inhibitory activity potentiated by 2.5 μM GSK2830371 in p53 wild-type (A375, WM35, C8161) but not p53 mutant (WM164, WM35-R, CHL-1) cutaneous melanoma cell lines by decreasing the GI50 of Siremadlin succinate[1].
Siremadlin succinate (72 h) had its cytotoxic activity potentiated by 2.5 μM GSK2830371 in p53 wild-type (A375, WM35, C8161) but not p53 mutant (WM164, WM35-R, CHL-1) cutaneous melanoma cell lines by decreasing the LC50 of Siremadlin (succinate)[1].
Siremadlin succinate(0.2 μM; 6 h, 24 h) in combination with 2.5 μM GSK2830371 enhances p53 stabilisation, phosphorylation, acetylation, and transcriptional activity in p53 wild-type (A375, C8161) cutaneous melanoma cell lines[1].
Siremadlin succinate (0.2 μM; 24 h) in combination with 2.5 μM GSK2830371 enhances p53-dependent cell cycle changes and apoptosis in p53 wild-type (A375, WM35, C8161) but not p53 mutant (WM35-R) cutaneous melanoma cell lines[1].
Siremadlin succinate had its activity potentiation by 2.5 μM GSK2830371 in p53 wild-type (A375, WM35) cutaneous melanoma cell lines strictly p53-dependent[1].

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

Siremadlin succinate Related Antibodies

Cell Proliferation Assay[1]

Cell Line: p53 wild-type (A375, WM35, C8161); p53 mutant (WM164, WM35-R, CHL-1) cutaneous melanoma cell lines
Concentration: 2.5 μM GSK2830371 (co-treatment)
Incubation Time: 72 h
Result: Significantly decreased the GI50 of HDM201 in p53 wild-type cutaneous melanoma cell lines compared to treatment with Siremadlin succinate alone.
Showed no potentiation in p53 mutant cell lines.\nSignificantly decreased the LC50 of siremadlin succinate in A375 and C8161 cells, and showed a similar trend in WM35 cells compared to treatment with Siremadlin (succinate) alone.
Showed no potentiation in p53 mutant cell lines.
Molecular Weight

673.50

Formula

C30H30Cl2N6O8
CAS No.
SMILES

OC(CCC(O)=O)=O.CC(N1C([C@H](C2=CC=C(C=C2)Cl)N3C4=CC(Cl)=CN(C)C4=O)=C(N=C1C5=CN=C(OC)N=C5OC)C3=O)C
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Room temperature in continental US; may vary elsewhere.
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References
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Siremadlin succinate 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:

Siremadlin1638193-48-2NVP-HDM201HDM201HDM 201HDM-201MDM-2/p53A375cell cycle distributionGSK2830371p53cutaneous melanoma cellsp53 wild-type cellsapoptotic responsesMDM2WIP1 inhibitorcaspase-3/7Inhibitorinhibitorinhibit

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