1. Epigenetics
  2. Histone Methyltransferase
  3. CARM1-IN-5

CARM1-IN-5 (Compound 17e) 是 CARM1 的高效选择性抑制剂 (IC50= 2 nM)。CARM1-IN-5 通过直接与 CARM1 相互作用,有效阻止其对底物蛋白进行甲基化。CARM1-IN-5 对黑色素瘤细胞系具有显著的抗增殖作用。

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CARM1-IN-5 Chemical Structure

CARM1-IN-5 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines[1].

体外研究
(In Vitro)

CARM1-IN-5 对 CARM1 具有选择性。IC50 分别为 2 ± 1 nM (CARM1), 213 ± 45 nM (PRMT1), 942 ± 78 nM (PRMT3), 64 ± 9 nM (PRMT6), 73 ± 8 nM (PRMT8), >100,000 nM (PRMT5), >100,000 nM (PRMT7)[1]
CARM1-IN-5 对两种黑色素瘤细胞系的抗增殖活性为 IC50 = 0.55 ± 0.03 μM (A375); 1.74 ± 0.07μM (A2058)[1]
CARM1-IN-5 (0-5 μM; 72 h) 可以进入 A375 Cells 并直接与 CARM1 结合。可以通过抑制 CARM1 的甲基转移酶活性,在细胞环境中影响 CARM1 底物的不对称二甲基化水平[1]



体外代谢稳定性[1]

t1/2 (min) Cl (mL/min/kg)
41.5 132

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

Western Blot Analysis[1]

Cell Line: A375 Cells
Concentration: 0; 0.3; 0.6; 1.2; 2.5; 5μM
Incubation Time: 72h
Result: Enhanced protein thermal stability of CARM1 in a concentration-dependent manner.
Reduced asymmetric dimethyl-PABP1 and overall aDMA levels in a dose-dependent manner.
体内研究
(In Vivo)

CARM1-IN-5 (i.p.; 10 mg/kg/day 和 25 mg/kg/day; 14 天) 显著抑制 BALB/c 皮下移植 A375 的裸鼠的肿瘤生长[1]

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

Animal Model: BALB/c nude mice bearing subcutaneous A375 xenograft [1]
Dosage: 10 mg/kg/daily; 25 mg/kg/daily for 14 days
Administration: i.p.
Result: TGI was 63% (25 mg/kg) and 55% (10 mg/kg).
Significantly reduced asymmetric dimethylation by western blotting.
分子量

431.98

Formula

C22H26ClN3O2S

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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CARM1-IN-5
目录号:
HY-158158
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