1. Apoptosis Epigenetics
  2. Apoptosis Histone Methyltransferase
  3. PRMT5-IN-33

PRMT5-IN-33 (compound A8) 是一种与 SAM 竞争的 PRMT5 选择性抑制剂,IC50 是 10.9 nM。PRMT5-IN-33 诱导细胞凋亡 (apoptosis) 并且抑制细胞 Z-138 和 MOLM-13 增殖。PRMT5-IN-33 有抗肿瘤活性。

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PRMT5-IN-33 Chemical Structure

PRMT5-IN-33 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity[1].

IC50 & Target[1]

PRMT5

10.9 nM (IC50)

PRMT1

6.89 μM (IC50)

体外研究
(In Vitro)

PRMT5-IN-33 抑制细胞 Z-138 和 MOLM-13 增殖,IC50 分别是 123.2 nM 和 248.6 nM[1]
PRMT5-IN-33 剂量依赖地降低 sDMA 水平[1]

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

Western Blot Analysis[1]

Cell Line: Z-138 and MOLM-13
Concentration: 50-500 nM
Incubation Time: 48 h
Result: Inhibited expression of sDMA.
体内研究
(In Vivo)

PRMT5-IN-33 (60-120 mg/kg,灌胃,一天两次,13天) 剂量依赖性地抑制 MOLM-13 异种移植肿瘤在 BALB/c 小鼠体内的生长,不引起体重减少[1]
PRMT5-IN-33 (口服,10 mg/kg,单次给药) 在 ICR 小鼠体内的药代动力学特征如下表所示[1]

PRMT5-IN-33 在 ICR 鼠体内的药代动力学特征[1]

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

route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) T1/2 (h)
po 10 0.25 6870 6730 6760 1.17
Animal Model: MOLM-13 xenograft tumor in nude BALB/c mice[1]
Dosage: 60-120 mg/kg
Administration: intragastrical administration (i.g.), twice a day for 13 days
Result: Exhibited a tumor growth inhibition rate (TGI) of 33% (60 mg/kg) and 52% (120 mg/kg)
分子量

554.46

Formula

C25H24BrN5O3S

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
PRMT5-IN-33
目录号:
HY-162230
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