PRMT Inhibitors

In recent years, the role of epigenetics in tumor initiation and progression has attracted extensive attention. In addition to genetic mutations, epigenetic alterations and post-translational modifications have been demonstrated to play crucial roles in cancer development and maintenance. Among these, protein arginine methyltransferases (PRMTs) represent an important family of epigenetic regulators that catalyze the methylation of arginine residues, thereby modulating gene expression, protein function, signal transduction, and cell cycle progression. To date, nine PRMT isoforms have been identified and are classified into three types based on their catalytic products: Type I PRMTs (e.g., PRMT1, PRMT4, PRMT6) generate asymmetric dimethylarginine (ADMA); Type II PRMTs (e.g., PRMT5, PRMT9) produce symmetric dimethylarginine (SDMA); and Type III PRMTs (e.g., PRMT7) catalyze monomethylarginine (MMA) formation. These enzymes act on both histone and non-histone substrates, establishing a complex regulatory network that integrates multiple cellular processes. Accumulating evidence indicates that PRMTs are overexpressed in various human cancers, including melanoma, multiple myeloma, glioblastoma, lung cancer, urothelial carcinoma of the bladder, gastric, cervical, ovarian, and colorectal cancers, and their dysregulation is closely associated with poor patient prognosis. Consequently, targeting PRMTs has emerged as a promising strategy for anticancer therapy. Notably, the biological effects of PRMT inhibition extend beyond chromatin regulation to RNA processing and immune signaling, providing unique therapeutic advantages and potential biomarker opportunities. Several PRMT inhibitors have demonstrated potent antitumor efficacy in preclinical and clinical studies. In the future, PRMT-targeted therapy is expected to be combined with DNMT, HDAC, or BET inhibitors, as well as DNA damage response modulators and immunotherapies, to achieve synergistic therapeutic outcomes. Collectively, PRMTs represent novel and compelling therapeutic targets with significant research and clinical potential in cancer treatment.

PRMT Inhibitors

TNG908
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A19386652760481-53-499%

TNG908

$1779.00/250mg Detail

PRMT6-IN-3
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A19641052890765-10-198%

PRMT6-IN-3

$97.00/10mg Detail

Onametostat
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A11764552086772-26-999%

Onametostat

$161.00/5mg Detail

PRMT4-IN-1
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A1953384912970-79-798%

PRMT4-IN-1

$452.00/5mg Detail

PRMT5-IN-49
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A1598855428853-17-298%

PRMT5-IN-49

$1009.00/1g Detail

MS023 2HCl
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A11773471992047-64-999+%

MS023 2HCl

$145.00/100mg Detail

CMP-5
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A1226665880813-42-398%

CMP-5

$239.00/50mg Detail

Furamidine 2HCl
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A50881955368-40-698%

Furamidine 2HCl

$168.00/25mg Detail

DCLX069
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A221373792946-69-195%

DCLX069

$554.00/5g Detail

SGC2085 HCl
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A12098471821908-49-999%

SGC2085 HCl

$84.00/1mg Detail

WDR5-0102
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A1921215824960-50-198%

WDR5-0102

$239.00/250mg Detail

TNG-462
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A24188472760483-96-198%

TNG-462

$157.00/10mg Detail

PR5-LL-CM01
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A14834551005307-86-798%

PR5-LL-CM01

$147.00/10mg Detail

Flavokawain A
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A6396303420-72-298%

Flavokawain A

$64.00/1g Detail

DS-437
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A13268101674364-87-498%

DS-437

$204.00/10mg Detail

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