ChemicalBook > CAS DataBase List > SP2509

SP2509

Product Name
SP2509
CAS No.
1423715-09-6
Chemical Name
SP2509
Synonyms
SP2509;CS-1755;HCI-2509;SP2509 ，S7680;SP 2509;SP-2509;SP-2509;HCI-2509;SP2509 USP/EP/BP;SP2509, 10 mM in DMSO;SP-2509, LSD1 inhibitor;LSD1 Inhibitor VII, SP-2509
CBNumber
CB22734796
Molecular Formula
C19H20ClN3O5S
Formula Weight
437.9
MOL File
1423715-09-6.mol
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SP2509 Property

Density 
1.44±0.1 g/cm3(Predicted)
storage temp. 
+2C to +8C
solubility 
Soluble in DMSO (up to at least 25 mg/ml)
form 
Off-white solid
pka
7.96±0.43(Predicted)
color 
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.09703
Product name
LSD1InhibitorVII,SP-2509-CAS1423715-09-6-Calbiochem
Packaging
10mg
Price
$220
Updated
2025/07/31
Cayman Chemical
Product number
15487
Product name
SP2509
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
15487
Product name
SP2509
Purity
≥98%
Packaging
5mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
15487
Product name
SP2509
Purity
≥98%
Packaging
10mg
Price
$153
Updated
2024/03/01
Cayman Chemical
Product number
15487
Product name
SP2509
Purity
≥98%
Packaging
25mg
Price
$343
Updated
2024/03/01
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SP2509 Chemical Properties,Usage,Production

Description

SP2509 (1423715-09-6) is a potent (IC50 = 13 nM) and reversible inhibitor of the histone demethylase LSD1 (KDM1A).1 It is inactive against the closely related flavin enzymes MAO A,B as well as lactate dehydrogenase, several CYP’s and hERG. LSD1 regulates the balance between self-renewal and differentiation of stem cells and is highly expressed in various cancers.2-6 SP2509 promotes autophagy in neuroblastoma cells.7

Uses

SP 2509 reduces the effect of the LSD1 binding to CoREST, resulting in increased methylation of H3K4 and driving increased expression of p21, p27 and CCAAT/enhancer binding protein α in acute myeloid leukemia cells. Anti-leukemia agent.

General Description

A cell-permeable, lysine-specific demethylase 1 (LSD1) active site-targeting phenethylidene-benzohydrazide that inhibits LSD1 activity (IC50 = 13 nM) in a reversible and substrate non-competitive (Ki = 34 nM) manner, while inhibiting CYP3A4 only at much higher concentrations (IC50 = 2.61 μM) and displaying little or no potency towards CYP1A2/2C9/2C19/2D6. MAO-A/B, D-lactate dehydrogenase, glucose oxidase, and hERG (IC50 ≥8.0 μM). Shown to enhance histone H3 Lys9 dimethylation (H3K9me2) in androgen-dependent prostate cancer VCaP cultures (1 to 10 μM) and effectively inhibits LSD1-dependent cancer growth (IC50 in nM = 329/SK-N-MC, 356/AN3 Ca, 429/HT29, 468/MIA PaCa-2, 489/BT-20, 612/HER218, 614/HCT 116, 637/MCF-7, 649/T-47D; 96 h).

Biochem/physiol Actions

Cell permeable: yes

in vivo

Treatment with SP2509 (25 mg/kg) and/or PS (5 mg/kg) significantly enhances PS-mediated loss of viability of CD34+ primary AML cells and improves the survival of mice bearing AML xenografts and primagrafts[2].

IC 50

KDM1/LSD1

References

[1] VENKATASWAMY SORNA. High-Throughput Virtual Screening Identifies Novel N′-(1-Phenylethylidene)-benzohydrazides as Potent, Specific, and Reversible LSD1 Inhibitors[J]. Journal of Medicinal Chemistry, 2013, 56 23: 9496-9508. DOI:10.1021/jm400870h
[2] AMIR HOSSEINI  Saverio M. A comprehensive review of lysine-specific demethylase 1 and its roles in cancer.[J]. Epigenomics, 2017, 9 8: 1123-1142. DOI:10.2217/epi-2017-0022
[3] W FISKUS. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells[J]. Leukemia, 2014, 28 11: 2155-2164. DOI:10.1038/leu.2014.119
[4] SHIJUN WEN . Novel combination of histone methylation modulators with therapeutic synergy against acute myeloid leukemia in vitro and in vivo[J]. Cancer letters, 2018, 413: Pages 35-45. DOI:10.1016/j.canlet.2017.10.015
[5] CHIA-LUNG TSAI. Stress-induced phosphoprotein 1 acts as a scaffold protein for glycogen synthase kinase-3 beta-mediated phosphorylation of lysine-specific demethylase 1.[J]. Oncogenesis, 2018: 31. DOI:10.1038/s41389-018-0040-z
[6] YUHONG LU. Hypoxia Promotes Resistance to EGFR Inhibition in NSCLC Cells via the Histone Demethylases, LSD1 and PLU-1.[J]. ACS Applied Energy Materials, 2018: 1458-1469. DOI:10.1158/1541-7786.mcr-17-0637
[7] S AMBROSIO. Lysine-specific demethylase LSD1 regulates autophagy in neuroblastoma through SESN2-dependent pathway[J]. Oncogene, 2017, 36 48: 6701-6711. DOI:10.1038/onc.2017.267

SP2509 Preparation Products And Raw materials

Raw materials

Preparation Products

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SP2509 Suppliers

China 115 India 1 United Kingdom 1 United States 16 Global 133
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Nanjing Dulai Biotechnology Co., Ltd.
Tel
025-846993838003-8003 18013301590
Fax
025-84699383-8003
Email
njduly@126.com
Country
China
ProdList
3249
Advantage
55
EnliPharma Technology Co., Ltd
Tel
0551-66399836 18955197623
Email
sales@enlipharma.com
Country
China
ProdList
1876
Advantage
55
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
Fax
+86-510-68873513
Country
China
ProdList
1785
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51395
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55

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  • 1423715-09-6
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