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^[1].

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.

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. 2783961-86-2 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 Data Sheet (275 KB) Handling Instructions (2659 KB) References [1]. Deqin Rong, et al. Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5. J Med Chem. 2022 Jun 9;65(11):7854-7875.  [Content Brief] [1]. Deqin Rong, et al. Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5. J Med Chem. 2022 Jun 9;65(11):7854-7875. Rating Lot Number * Submit an Image No file chosen (Maximum size is: 1024 Kb) PubMed ID If you have published this work, please enter the PubMed ID. Show My Name Your name will appear on the site. Email Remarks PRMT5-IN-19 Related Classifications Cancer Cancer Targeted Therapy Cancer Metabolism and Metastasis Epigenetics Histone Methyltransferase Molarity Calculator Dilution Calculator The molarity calculator equation Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass   Concentration   Volume   Molecular Weight * kg g mg μg ng pg = M mM μM nM pM × L mL μL × The dilution calculator equation Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 Concentration (start) × Volume (start) = Concentration (final) × Volume (final) M mM μM nM pM × L mL μL = M mM μM nM pM × L mL μL 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. 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