Date published: 2025-11-1

1-800-457-3801

SCBT Portrait Logo
Seach Input

UNC0631 (CAS 1320288-19-4)

0.0(0)
Write a reviewAsk a question

Alternate Names:
N-[1-(Cyclohexylmethyl)-4-piperidinyl]-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
Application:
UNC0631 is a selective histone lysine methyltransferase (HMTase) inhibitor
CAS Number:
1320288-19-4
Molecular Weight:
635.93
Molecular Formula:
C37H61N7O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

QUICK LINKS

UNC0631 demonstrates remarkable potency and selectivity as an inhibitor of G9a activity both in vitro and in cellular contexts. In vitro, it exhibits a potent inhibitory effect on G9a activity with an IC50 of 4 nM, effectively impeding G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells with an IC50 of 25 nM. Its inhibitory prowess extends to various cancer cell lines and the human fetal lung IMR-90 cell line, effectively targeting G9a/GLP activity. UNC0631 stands out as a novel G9a inhibitor, showcasing exceptional potency across multiple cell lines while maintaining a significant separation between functional efficacy and cellular toxicity. The protein lysine methyltransferase G9a plays a pivotal role in transcriptional repression, employing H3K9me2 dimethylation of chromatin as well as nonhistone proteins.


UNC0631 (CAS 1320288-19-4) References

  1. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.  |  Liu, F., et al. 2011. J Med Chem. 54: 6139-50. PMID: 21780790
  2. The H3K9 Methyltransferase G9a Represses E-cadherin and is Associated with Myometrial Invasion in Endometrial Cancer.  |  Hsiao, SM., et al. 2015. Ann Surg Oncol. 22 Suppl 3: S1556-65. PMID: 25613390
  3. Histone demethylase KDM3A is required for enhancer activation of hippo target genes in colorectal cancer.  |  Wang, HY., et al. 2019. Nucleic Acids Res. 47: 2349-2364. PMID: 30649550
  4. Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents.  |  Cao, H., et al. 2019. Eur J Med Chem. 179: 537-546. PMID: 31276898
  5. The Histone Methyltransferase G9a Promotes Cholangiocarcinogenesis Through Regulation of the Hippo Pathway Kinase LATS2 and YAP Signaling Pathway.  |  Ma, W., et al. 2020. Hepatology. 72: 1283-1297. PMID: 31990985
  6. Upregulation of miR-101a Suppresses Chronic Renal Fibrosis by Regulating KDM3A via Blockade of the YAP-TGF-β-Smad Signaling Pathway.  |  Ding, H., et al. 2020. Mol Ther Nucleic Acids. 19: 1276-1289. PMID: 32092824
  7. Chaetocin Abrogates the Self-Renewal of Bladder Cancer Stem Cells via the Suppression of the KMT1A-GATA3-STAT3 Circuit.  |  Yang, Z., et al. 2020. Front Cell Dev Biol. 8: 424. PMID: 32626701
  8. Activity Comparison of Epigenetic Modulators against the Hemoprotozoan Parasites Babesia divergens and Plasmodium falciparum.  |  Vanheer, LN. and Kafsack, BFC. 2021. ACS Infect Dis. 7: 2277-2284. PMID: 33599488
  9. High-Throughput Mechanistic Screening of Epigenetic Compounds for the Potential Treatment of Meningiomas.  |  Tatman, PD., et al. 2021. J Clin Med. 10: PMID: 34300316
  10. Histone demethylase KDM3C regulates the lncRNA GAS5-miR-495-3p-PHF8 axis in cardiac hypertrophy.  |  Zhao, L., et al. 2022. Ann N Y Acad Sci. 1516: 286-299. PMID: 35777757
  11. Augmented Production of Platelets From Cord Blood With Euchromatic Histone Lysine Methyltransferase Inhibition.  |  Liu, Y., et al. 2022. Stem Cells Transl Med. 11: 946-958. PMID: 35880582
  12. KDM3A promotes oral squamous cell carcinoma cell proliferation and invasion via H3K9me2 demethylation-activated DCLK1.  |  Yang, L., et al. 2022. Genes Genomics. 44: 1333-1342. PMID: 36094735
  13. Synergistic Effect of Combined Inhibition of the Checkpoint kinase 1 and G9a Methyltransferase Pathways in Pancreatic Cancer  |  Urrutia, G., Salmonson, A., & Lomberk, G. 2018. The FASEB Journal. 32: 835.1-835.1.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

UNC0631, 5 mg

sc-397011
5 mg
$149.00