1. Apoptosis Epigenetics
  2. Histone Methyltransferase Apoptosis
  3. Antiproliferative agent-25

Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes.

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Antiproliferative agent-25

Antiproliferative agent-25 Chemical Structure

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Description

Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes[1].

IC50 & Target

0.11 μM (PRMT5)[1]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
14.25 μM
Compound: 3s4
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
[PMID: 37429083]
HepG2 IC50
58.14 μM
Compound: 3s4
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
[PMID: 37429083]
L02 IC50
> 100 μM
Compound: 3s4
Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
[PMID: 37429083]
MCF7 IC50
28.89 μM
Compound: 3s4
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
[PMID: 37429083]
MDA-MB-231 IC50
21.33 μM
Compound: 3s4
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by SRB assay
[PMID: 37429083]
Molecular Weight

401.30

Formula

C20H21BrN2O2

SMILES

O[C@@H](CN1C=CC2=C1C=C(Br)C=C2)CN(C3)CCC4=C3C=CC(O)=C4

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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Product Name:
Antiproliferative agent-25
Cat. No.:
HY-155051
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