2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. SKLB-03220

SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer.

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SKLB-03220

SKLB-03220 Chemical Structure

CAS No. : 2852050-29-2

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SKLB-03220 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer[1].

IC50 & Target[1]

EZH2 WT

1.72 nM (IC50)

EZH2 Y641N

 

EZH2 Y641F mutant type

 

In Vitro

SKLB-03220 (0.5-10 μM, 3-14 days) inhibits PA-1 and A2780 cell proliferation and colony formation[1].
SKLB-03220 (5-40 μM, 48 h) induces apoptosis of PA-1 cells[1].
SKLB-03220 (0-5 μM, 0-4 d) inhibits the expression of H3K27me3 in PA-1 cells[1].
SKLB-03220 (10 μM, 3 d + washout 0-4 d) achieves persistent target inhibition and long-lasting anti-tumor effects in PA-1 cells[1].

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

SKLB-03220 Related Antibodies

Apoptosis Analysis[1]

Cell Line: PA-1 cells
Concentration: 5, 10, 20 and 40 μM
Incubation Time: 48 h
Result: Induced ovarian cancer cell apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: PA-1 cells
Concentration: 0, 0.3, 0.6, 1.2, 2.5 and 5 μM
Incubation Time: 0, 1, 2, 3, 4 d
Result: Effectively and persistently reduced the level of H3K27me3 within the cells, without affecting the total protein quantity of EZH2.
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 100 mg/kg p.o. Cmax 6740.93 ng/mL
Rat 5 mg/kg i.v. Cmax 22792.57 ng/mL
Rat 100 mg/kg p.o. Tmax 0.38 h
Rat 5 mg/kg i.v. Tmax 0.08 h
Rat 100 mg/kg p.o. T1/2 0.77 h
Rat 5 mg/kg i.v. T1/2 0.61 h
Rat 100 mg/kg p.o. AUC0-t 12615.91 μg/L·h
Rat 5 mg/kg i.v. AUC0-t 7725.47 μg/L·h
Rat 100 mg/kg p.o. MRT0-t 1.73 h
Rat 5 mg/kg i.v. CL 699.32 mL/min/kg
Rat 100 mg/kg p.o. F 8.73 %
Rat 5 mg/kg i.v. Vss 202.28 mL/kg
Rat 5 mg/kg i.v. MRT0-t 0.26 h
In Vivo

SKLB-03220 (75-150 mg/kg, p.o., twice daily for 21 days) significantly inhibits tumor growth and with good tolerance in PA-1 cells xenograft mice model[1].

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

Animal Model: PA-1 cells xenograft model established in BALB/C nude mice (6 weeks)[1]
Dosage: 75 and 150 mg/kg
Administration: Oral administration (p.o.), twice daily for 21 days
Result: Significantly inhibits tumor growth in a dose-dependent manner.
Reduced the Ki-67 and H3K27me3 signals and increased cleaved Caspase-3 in tumor tissues.
No significant abnormalities were observed in terms of body weight, blood routine, blood biochemical indicators, and pathological sections of major organs.
Molecular Weight

556.70

Formula

C33H40N4O4
CAS No.
SMILES

O=C(NC1=CC=C(C)C(C2=CC(N(C3CCOCC3)CC)=C(C)C(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2)=C1)C=C
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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SKLB-03220 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:

SKLB-032202852050-29-2SKLB03220SKLB 03220Histone MethyltransferaseApoptosisCovalent InhibitorPA-1 cellsmice modelH3K27me3PharmacokineticsInhibitorinhibitorinhibit

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