2. Epigenetics GPCR/G Protein
  3. Histone Methyltransferase GLP Receptor
  4. Antitumor agent-101

Antitumor agent-101 是赖氨酸甲基转移酶 G9a/GLP 的选择性共价抑制剂，对 G9a 和 GLP 的 IC50 分别为 8.5 nM 和 5.5 nM。Antitumor agent-101 在 PANC-1 异种移植模型中显示出抗肿瘤效果。

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Antitumor agent-101 Chemical Structure

Antitumor agent-101 Chemical Structure

CAS No. : 2848632-52-8

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Antitumor agent-101 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 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

Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model[1].

IC50 & Target[1]

G9a

8.5 nM (IC50)

GLP

5.5 nM (IC50)

体外研究
(In Vitro)

Antitumor agent-101 (Compound 27) ( 0-5 μM；48 小时) 抑制 PANC-1 和 MDA-MB-231 细胞的增殖和克隆形成[1]。
Antitumor agent-101 ( 0-10 μM；0-96 小时) 以浓度和时间依赖性方式有效降低 PANC-1 和 MDA-MB-231 细胞中的 H3K9me2 水平。

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

Antitumor agent-101 相关抗体:

Cell Proliferation Assay[1]

Cell Line: PANC-1 and MDA-MB-231 cells
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 48 hours
Result: Ihibited proliferation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively.
Significantly suppressed the colony formation in MDA-MB-231 and PANC-1 cell lines at 2.5 μM.

Western Blot Analysis[1]

Cell Line: PANC-1 and MDA-MB-231 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 4, 48, 72, or 96 hours
Result: Effectively reduced H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner.
Still significantly inhibited the levels of H3K9me2 in the cells treated with compound 27 were still significantly inhibited within 24h after Antitumor agent-101 was washed out, and the levels of H3K9me2 were recovered after 48h.
体内研究
(In Vivo)

Antitumor agent-101 (Compound 27) (2 mg/kg，腹腔注射，每周五天) 通过抑制 G9a/GLP 的甲基转移酶活性来抑制 PANC-1 异种移植肿瘤的生长[1]。
Antitumor agent-101 (2 mg/kg，腹腔注射) 显示 Cmax 为 316 ng/mL，平均停留时间 (MRT) 为 0.61 小时[1]。

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

Animal Model: PANC-1 xenograft tumor models in male Balb/c nu/nu mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), 5 days a week (5 days on and 2 days off).
Result: Exhibited potent antitumor activity with a tumor growth inhibition (TGI) rate of 52.2% with no obvious toxicity.
Showed lower levels of H3K9me2 than the vehicle group.
Animal Model: Male ICR Mice (Pharmacokinetic assay)[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Pharmacokinetic parameters for antitumor agent-101 (Compound 27) in rats [1]
Route Dose (mg/kg) Cmax (ng/mL) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) MRT (h)
i.p. 2 316 208 214 0.61
分子量

482.62

Formula

C26H38N6O3
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

Antitumor agent-101 相关分类

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  • 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:

Antitumor agent-1012848632-52-8Antitumor agent101Antitumor agent 101Histone MethyltransferaseGLP ReceptorProtein lysine methyltransferasesG9aGLPPANC-1 xenograft modeMDA-MB-231 cellsInhibitorinhibitorinhibit

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