SKLB-03220

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SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC₅₀ of 1.72 nM for EZH2^MUT. 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.

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

SKLB-03220 Chemical Structure

CAS No. : 2852050-29-2

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•Related Small Molecules:

•Related Proteins:

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 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

EZH2 WT

1.72 nM (IC₅₀)

EZH2 Y641N

EZH2 Y641F mutant type

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	24.5 μM Compound: 12d; SKLB-03220	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A2780	IC₅₀	11.2 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	IC₅₀	28.7 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
BT-549	IC₅₀	18.9 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
ES-2	IC₅₀	36.4 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
HEY	IC₅₀	35.5 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
MCF7	IC₅₀	56.2 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
NCI-H1703	IC₅₀	26.3 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OAW-42	IC₅₀	> 100 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OVCAR-3	IC₅₀	35.6 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PA-1	IC₅₀	10.1 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SK-BR-3	IC₅₀	22.8 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SK-OV-3	IC₅₀	56.4 μM Compound: 12d; SKLB-03220	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]

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.

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

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	MRT_0-t	F	CL	V_ss
Rat^[1]	100 mg/kg	p.o.	6740.93 ng/mL	0.38 h	0.77 h	12615.91 μg/L·h	1.73 h	8.73 %	/	/
Rat^[1]	5 mg/kg	i.v.	22792.57 ng/mL	0.08 h	0.61 h	7725.47 μg/L·h	0.26 h	/	699.32 mL/min/kg	202.28 mL/kg

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.

2852050-29-2

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

Handling Instructions (2659 KB)

References

[1]. Zhang Q, et al. Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. J Med Chem. 2023 Feb 9;66(3):1725-1741. [Content Brief]

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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