2. Cell Cycle/DNA Damage Apoptosis
  3. Wee1 Apoptosis
  4. PKMYT1-IN-10

PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.

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PKMYT1-IN-10

PKMYT1-IN-10 Chemical Structure

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PKMYT1-IN-10 Related Antibodies

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PKMYT1

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Description

PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer[1].

IC50 & Target[1]

PKMYT1

3 nM (IC50)

In Vitro

PKMYT1-IN-10 (Compound A30) demonstrates potent cytostatic activity, with IC50 values of 0.32 μM, 0.33 μM, and > 8 μM in the OVCAR3, HCC1569 and A549 cell lines, respectively[1].
PKMYT1-IN-10 (0.125-2 μM, 14 days) inhibits colony formation in the OVCAR3 and HCC1569 cells with EC50s of 0.37 and 0.35 μM[1].
PKMYT1-IN-10 (0.3-2.4 μM, 5 days) induces HCC1569 cells apoptosis and induces S-phase-specific cell cycle arrest in HCC1569 cells and OVCAR3 cells[1].
PKMYT1-IN-10 (37.5-600 nM) shows a high degree of synergy with Gemcitabine (HY-17026) with combination index (CI) values of < 0.5 and 0.5-0.8 in HCC1569 cells and OVCAR3 cells, respectively[1].

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

PKMYT1-IN-10 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCC1569 cells
Concentration: 0.3, 0.6 and 1.2 μM
Incubation Time: 5 days
Result: Reached the apoptosis rate by 54.7% at a concentration of 2.4 μM in HCC1569 cells.

Cell Cycle Analysis[1]

Cell Line: HCC1569 cells and OVCAR3 cells
Concentration: 0.3, 0.6 and 1.2 μM
Incubation Time: 5 days
Result: Increased the proportion of cells in the S phase, without causing the typical G2/M arrest.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 3 mg/kg i.v. T1/2 0.20 h
Mice 30 mg/kg p.o. T1/2 0.70 h
Mice 3 mg/kg i.v. Tmax 0.08 h
Mice 30 mg/kg p.o. Tmax 0.33 h
Mice 3 mg/kg i.v. Cmax 622 ng/mL
Mice 30 mg/kg p.o. Cmax 721 ng/mL
Mice 3 mg/kg i.v. AUC0-t 188 ng·h/mL
Mice 30 mg/kg p.o. AUC0-t 497 ng·h/mL
Mice 3 mg/kg i.v. AUC0-∞ 191 ng·h/mL
Mice 30 mg/kg p.o. AUC0-∞ 504 ng·h/mL
Mice 3 mg/kg i.v. MRT0-t 0.12 h
Mice 30 mg/kg p.o. MRT0-t 0.57 h
Mice 3 mg/kg i.v. MRT0-∞ 0.14 h
Mice 30 mg/kg p.o. MRT0-∞ 0.63 h
Mice 3 mg/kg i.v. Vz 4584 mL/kg
Mice 30 mg/kg p.o. F 26.44 %
Mice 3 mg/kg i.v. CL 263 mL/min/kg
Molecular Weight

453.51

Formula

C22H23N5O4S
SMILES

O=C(C1=CN=C(NC2=CC=C(S(=O)(C3CC3)=O)C=C2)N=C1N)NC4=C(C)C=CC(O)=C4C
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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PKMYT1-IN-10 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:

PKMYT1-IN-10Wee1Apoptosisovarian cancerbreast cancerapoptosisOVCAR3 cellsHCC1569 cellsInhibitorinhibitorinhibit

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