SP-2509
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406610

CAS#: 1423715-09-6

Description: SP-2509 is a novel histone demethylase LSD1 inhibitor, which showed high actitivity on human AML cells. Treatment with the novel LSD1 antagonist SP2509 attenuated the binding of LSD1 with the corepressor CoREST, increased the permissive H3K4Me3 mark on the target gene promoters, and increased the levels of p21, p27 and CCAAT/enhancer binding protein α in cultured AML cells. In addition, SP2509 treatment or LSD1 shRNA inhibited the colony growth of AML cells.


Chemical Structure

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SP-2509
CAS# 1423715-09-6

Theoretical Analysis

MedKoo Cat#: 406610
Name: SP-2509
CAS#: 1423715-09-6
Chemical Formula: C19H20ClN3O5S
Exact Mass: 437.08
Molecular Weight: 437.900
Elemental Analysis: C, 52.11; H, 4.60; Cl, 8.10; N, 9.60; O, 18.27; S, 7.32

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
1g USD 3850 Ready to ship
2g USD 6550 Ready to ship
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Synonym: SP2509; SP 2509; SP-2509.

IUPAC/Chemical Name: (E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide.

InChi Key: NKUDGJUBIVEDTF-FYJGNVAPSA-N

InChi Code: InChI=1S/C19H20ClN3O5S/c1-13(17-12-15(20)5-6-18(17)24)21-22-19(25)14-3-2-4-16(11-14)29(26,27)23-7-9-28-10-8-23/h2-6,11-12,24H,7-10H2,1H3,(H,22,25)/b21-13+

SMILES Code: O=C(N/N=C(C1=CC(Cl)=CC=C1O)\C)C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Biological target: SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM.
In vitro activity: SP-2509 may have therapeutic potential in the treatment of herpes. Treatment of herpes simplex virus 1 (HSV-1)-infected cells with SP-2509 blocked viral DNA replication, gene expression after the onset of DNA replication, and virus production. However, SP-2509 did not inhibit HSV-1 IE gene expression or transcription factor and RNA polymerase II (Pol II) association with viral DNA prior to the onset of replication. Reference: J Virol. 2020 Sep 15;94(19):e00974-20. https://pubmed.ncbi.nlm.nih.gov/32699090/
In vivo activity: The combination of SP-2509 and panobinostat is a promising therapy warranting further testing against acute myeloid leukemia (AML). Treatment with SP-2509 alone significantly improved the survival of immune-depleted mice following tail-vein infusion and engraftment of cultured or primary human AML cells. However, co-treatment with SP-2509 and panobinostat significantly improved the survival of the mice engrafted with the human AML cells, without exhibiting any toxicity. Reference: Leukemia. 2014 Nov;28(11):2155-64. https://pubmed.ncbi.nlm.nih.gov/24699304/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.0 75.36

Preparing Stock Solutions

The following data is based on the product molecular weight 437.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Harancher MR, Packard JE, Cowan SP, DeLuca NA, Dembowski JA. Antiviral Properties of the LSD1 Inhibitor SP-2509. J Virol. 2020 Sep 15;94(19):e00974-20. doi: 10.1128/JVI.00974-20. PMID: 32699090; PMCID: PMC7495396. 2. Wang J, Yu Q, Qiu Z, Dai T, Wang S, Yang X, Evers BM, Wu Y. The combined effect of epigenetic inhibitors for LSD1 and BRD4 alters prostate cancer growth and invasion. Aging (Albany NY). 2020 Jan 5;12(1):397-415. doi: 10.18632/aging.102630. Epub 2020 Jan 5. PMID: 31901895; PMCID: PMC6977660. 3. Khanal T, Choi K, Leung YK, Wang J, Kim D, Janakiram V, Cho SG, Puga A, Ho SM, Kim K. Loss of NR2E3 represses AHR by LSD1 reprogramming, is associated with poor prognosis in liver cancer. Sci Rep. 2017 Sep 6;7(1):10662. doi: 10.1038/s41598-017-11106-2. PMID: 28878246; PMCID: PMC5587550. 4. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D, Bhalla KN. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64. doi: 10.1038/leu.2014.119. Epub 2014 Apr 4. Erratum in: Leukemia. 2017 Jul;31(7):1658. PMID: 24699304; PMCID: PMC4739780.
In vitro protocol: 1. Harancher MR, Packard JE, Cowan SP, DeLuca NA, Dembowski JA. Antiviral Properties of the LSD1 Inhibitor SP-2509. J Virol. 2020 Sep 15;94(19):e00974-20. doi: 10.1128/JVI.00974-20. PMID: 32699090; PMCID: PMC7495396. 2. Wang J, Yu Q, Qiu Z, Dai T, Wang S, Yang X, Evers BM, Wu Y. The combined effect of epigenetic inhibitors for LSD1 and BRD4 alters prostate cancer growth and invasion. Aging (Albany NY). 2020 Jan 5;12(1):397-415. doi: 10.18632/aging.102630. Epub 2020 Jan 5. PMID: 31901895; PMCID: PMC6977660.
In vivo protocol: 1. Khanal T, Choi K, Leung YK, Wang J, Kim D, Janakiram V, Cho SG, Puga A, Ho SM, Kim K. Loss of NR2E3 represses AHR by LSD1 reprogramming, is associated with poor prognosis in liver cancer. Sci Rep. 2017 Sep 6;7(1):10662. doi: 10.1038/s41598-017-11106-2. PMID: 28878246; PMCID: PMC5587550. 2. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D, Bhalla KN. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64. doi: 10.1038/leu.2014.119. Epub 2014 Apr 4. Erratum in: Leukemia. 2017 Jul;31(7):1658. PMID: 24699304; PMCID: PMC4739780.

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 1: Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D,  Bhalla KN. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64. doi: 10.1038/leu.2014.119. Epub 2014 Apr 4. PubMed PMID: 24699304.