SP2509 (CAS 1423715-09-6)
CAS Number:
1423715-09-6
Molecular Weight:
437.9
Molecular Formula:
C19H20ClN3O5S
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SP2509 is a selective and reversible inhibitor of lysine-specific demethylase 1 (LSD1), a protein involved in demethylating histone H3 lysine 4 (H3K4). By inhibiting LSD1, SP2509 prevents the removal of methyl groups from H3K4, leading to transcriptional repression. This novel LSD1 inhibitor has a high potency, with an IC50 value of 13 nM. Notably, SP2509 does not affect the activity of monoamine oxidases A and B. In cultured acute myeloid leukemia (AML) cells, SP2509 disrupts the interaction between LSD1 and its co-repressor CoREST. Consequently, the methylation of H3K4 is increased, resulting in enhanced expression of key regulatory genes such as p21, p27, and CCAAT/enhancer binding protein α.
SP2509 (CAS 1423715-09-6) References
- Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. | Fiskus, W., et al. 2014. Leukemia. 28: 2155-64. PMID: 24699304
- Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target. | Inui, K., et al. 2017. Protein Sci. 26: 997-1011. PMID: 28218430
- Lysine-specific demethylase LSD1 regulates autophagy in neuroblastoma through SESN2-dependent pathway. | Ambrosio, S., et al. 2017. Oncogene. 36: 6701-6711. PMID: 28783174
- Loss of NR2E3 represses AHR by LSD1 reprogramming, is associated with poor prognosis in liver cancer. | Khanal, T., et al. 2017. Sci Rep. 7: 10662. PMID: 28878246
- LSD1 (KDM1A)-independent effects of the LSD1 inhibitor SP2509 in cancer cells. | Sonnemann, J., et al. 2018. Br J Haematol. 183: 494-497. PMID: 29205263
- Suppression of LSD1 enhances the cytotoxic and apoptotic effects of regorafenib in hepatocellular carcinoma cells. | Wu, LW., et al. 2019. Biochem Biophys Res Commun. 512: 852-858. PMID: 30929918
- LSD1 inhibition suppresses the growth of clear cell renal cell carcinoma via upregulating P21 signaling. | Zhu, L., et al. 2019. Acta Pharm Sin B. 9: 324-334. PMID: 30972280
- Epigenetic drug library screening identified an LSD1 inhibitor to target UTX-deficient cells for differentiation therapy. | Wu, B., et al. 2019. Signal Transduct Target Ther. 4: 11. PMID: 31044091
- Small molecule inhibition of lysine-specific demethylase 1 (LSD1) and histone deacetylase (HDAC) alone and in combination in Ewing sarcoma cell lines. | Welch, D., et al. 2019. PLoS One. 14: e0222228. PMID: 31550266
- The Histone Lysine-specific Demethylase 1 Inhibitor, SP2509 Exerts Cytotoxic Effects against Renal Cancer Cells through Downregulation of Bcl-2 and Mcl-1. | Wu, K., et al. 2020. J Cancer Prev. 25: 79-86. PMID: 32647649
- Antiviral Properties of the LSD1 Inhibitor SP-2509. | Harancher, MR., et al. 2020. J Virol. 94: PMID: 32699090
- SP2509, an inhibitor of LSD1, exerts potential antitumor effects by targeting the JAK/STAT3 signaling. | Zhen, H., et al. 2021. Acta Biochim Biophys Sin (Shanghai). 53: 1098-1105. PMID: 34169322
- Intermolecular insights into allosteric inhibition of histone lysine-specific demethylase 1. | Zhang, X., et al. 2021. Biochim Biophys Acta Gen Subj. 1865: 129990. PMID: 34390793
- SP2509, a Selective Inhibitor of LSD1, Suppresses Retinoblastoma Growth by Downregulating β-catenin Signaling. | Jiang, A., et al. 2022. Invest Ophthalmol Vis Sci. 63: 20. PMID: 35297943
- JAK/BCL2 inhibition acts synergistically with LSD1 inhibitors to selectively target ETP-ALL. | Benyoucef, A., et al. 2022. Leukemia. 36: 2802-2816. PMID: 36229595
Inhibitor of:
2200001I15Rik, AOF1, B7-H3, BC060267, BMAL2, C230097I24Rik, C6orf150, C9orf69, COL20A1, COL4A, Cytokeratin 12, E230028L10Rik, EG245440, EG270499, EG382265, EG432838, HIPK2, Id2, JMJD1B, JMJD1C, JMJD4, KDM (lysine demethylase), Klotho, LOC100039995, LSD1, LysRS, MUP20, Nkx-2.5, Nrarp, Olfr481, Olfr552, Olfr630, OTTMUSG00000007521, OTTMUSG00000007655, PHC3, PRDM12, RBM42, SmcX, TAP, VPS72, Wnt-14b, and ZBTB2.Activator of:
ARID2, BC061237, C23, CMV pp65, Cypt3, DDX56, E130012A19Rik, IL-7, LSD1, Paf1, PALB2, Pdcd-1L1, and USP9X.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SP2509, 5 mg | sc-492604 | 5 mg | $284.00 |