SP-2509 | CAS#1423715-09-6 | LSD1 inhibitor

MedKoo Cat#: 406610 | Name: SP-2509

Description:

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

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

SP-2509

CAS#1423715-09-6

Theoretical Analysis

MedKoo Cat#: 406610

Name: SP-2509

CAS#: 1423715-09-6

Chemical Formula: C19H20ClN3O5S

Exact Mass: 437.0812

Molecular Weight: 437.90

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
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,650.00	Ready to ship
1g	USD 3,850.00	Ready to ship
2g	USD 6,550.00	Ready to ship

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Related CAS #

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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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C20R06B24

QC Data

View QC data: current batch, Lot#C20R06B24

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	33.0	75.36

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.