2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT5-IN-19

PRMT5-IN-19 (Compound 41) 是一种具有口服活性的非核苷 PRMT5 选择性抑制剂，IC50 值为 23.9 nM (radioactive biochemical assay), 47 nM (AlphaLISA assay)。PRMT5-IN-19 可占据 PRMT5 中的 SAM-binding pocket 并封闭甲基转移酶的活性，选择性优于 PRMTs 和 PKMTs。PRMT5-IN-19 通过诱导细胞凋亡 (apoptosis) 来抑制细胞增殖，可用于癌症相关研究。

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PRMT5-IN-19 Chemical Structure

PRMT5-IN-19 Chemical Structure

CAS No. : 2783961-86-2

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PRMT5-IN-19 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

PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research[1].

IC50 & Target

PRMT5

23.9 nM (IC50)

PRMT1

3.252 μM (IC50)

PRMT4

>20 μM (IC50)

体外研究
(In Vitro)

PRMT5-IN-19 (Compound 41, 5 days) has strong anti-proliferative effects against the A375 cell with an IC50 value of 1.36 μM[1].
PRMT5-IN-19 shows higher selectivity for PRMT5 (IC50 value of 23.9 nM) than other histone methyltransferases (PRMT1 and PRMT4), and PKMTS (EZH2, NSD2, MLL1, and MLL4) [1].
PRMT5-IN-19 binds with the SAM-binding pocket in PRMT5[1].
PRMT5-IN-19 (4-5 days) Inhibits proliferation of multiple cancer cell lines (A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13) with IC50 value ranging from 1.08 to 3.45 μM[1].
PRMT5-IN-19 inhibits arginine symmetrical dimethylation in A375 cells [1].
PRMT5-IN-19 (0-4 μM, 48 h) suppresses A375 cell proliferation by inducing apoptosis in a concentration-dependent manner[1].

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

PRMT5-IN-19 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13
Concentration: 0-10 μM
Incubation Time: 5 days
Result: Inhibited proliferation of multiple cancer cell lines with IC50 value ranging from 1.08 to 3.45 μM.

Western Blot Analysis[1]

Cell Line: A-375 cells
Concentration: 0.5, 1, 2, 4,8 μM
Incubation Time: 48 h.
Result: Inhibited arginine symmetrical dimethylation in a dose-dependent manner.
体内研究
(In Vivo)

PRMT5-IN-19 (Compound 41, A375 xenograft model, 75 mg/kg/d, p.o., 19 days) has good PK properties and significant antitumor efficacy, without the obvious loss of body weight and visible toxicity[1].

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

Animal Model: A375 cell-derived nude mouse xenograft model[1].
Dosage: 75 mg/kg/d
Administration: P.o., 19 days
Result: Had no effect on the body weight, displayed antitumor efficacy with a tumor growth inhibition (TGI) rate of 73% by inhibiting the methyltransferase activity of PRMT5.
Animal Model: Rats and mice[1].
Dosage: 10 mg/kg for p.o., 3 mg/kg for i.v
Administration: P.o., i.v. (Pharmacokinetic Analysis)
Result: Pharmacokinetic parameters for PRMT5-IN-19 in SD Rats and Micea,c [1].
species PRMT5-IN-19 T1/2 (h) Cmax (ng/mL) CL (mL/min/kg) F (%)
rat iv (3 mg/kg)/td> 2.58 310
po (10 mg/kg)/td> 7.51 8.22 7.25
po (10 mg/kg)/td> 2.95 27.7 23.7
mouse iv (3 mg/kg)/td> 4.71 153
po (10 mg/kg)/td> 128
分子量

396.48

Formula

C25H24N4O
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

PRMT5-IN-19 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:

PRMT5-IN-192783961-86-2Histone MethyltransferaseA375 cellSAM-binding pocketmethyltransferasecell apoptosisA375 xenograft modelcancerInhibitorinhibitorinhibit

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