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

SKLB-03220 是一种具有选择性且口服有效的 EZH2 共价抑制剂，对 EZH2MUT 的 IC50 为 1.72 nM。SKLB-03220 对其他的组蛋白甲基转移酶 (HMT) 和激酶表现出较弱的活性。SKLB-03220 对卵巢癌细胞系表现出显著的抑制作用，并诱导了细胞凋亡 (apoptosis)。SKLB-03220 在 PA-1 异种移植模型中显著抑制肿瘤生长。SKLB-03220 可用于卵巢癌的研究。

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SKLB-03220

SKLB-03220 Chemical Structure

CAS No. : 2852050-29-2

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SKLB-03220 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

SKLB-03220 (0.5-10 μM，3-14 天) 可抑制 PA-1 和 A2780 细胞增殖和集落形成[1]。
SKLB-03220 (5-40 μM，48 小时) 可诱导 PA-1 细胞凋亡[1]。
SKLB-03220 (0-5 μM，0-4 天) 可抑制 PA-1 细胞中 H3K27me3 的表达[1]。
SKLB-03220 (10 μM，3 天 + 洗脱 0-4 天) 在 PA-1 细胞中实现持续的靶向抑制和持久的抗肿瘤作用[1]。

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

SKLB-03220 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

SKLB-03220 (75-150 mg/kg，口服，每日两次，持续 21 天) 显著抑制肿瘤生长，并在 PA-1 细胞异种移植小鼠模型中表现出良好的耐受性[1]。

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.
分子量

556.70

Formula

C33H40N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SKLB-03220 相关分类

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  • 稀释计算器

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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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产品名称：
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目录号：
HY-177497
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