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

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.

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PRMT5-IN-19 Chemical Structure

PRMT5-IN-19 Chemical Structure

CAS No. : 2783961-86-2

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Description

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)

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].

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

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.
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].

MedChemExpress (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
Molecular Weight

396.48

Formula

C25H24N4O

CAS No.
SMILES

C[C@H](OC1=CC=C(C2=CC3=C(N=CN=C3N2)C4=CCNCC4)C=C1)C5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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HY-149005
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