SP2509

ChemicalBook > CAS DataBase List > SP2509

Product Name: SP2509
CAS No.: 1423715-09-6
Chemical Name: SP2509
Synonyms: SP2509;CS-1755;HCI-2509;SP 2509;SP-2509;SP-2509;HCI-2509;SP2509 USP/EP/BP;(E)-N'-(1-(5-Chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide;(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide;3-(4-Morpholinylsulfonyl)benzoic acid (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide;Benzoic acid, 3-(4-morpholinylsulfonyl)-, (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide
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: $252
Updated: 2024/03/01

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 (K_i = 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

References

1) Sorna, et al. (2013), High-Throughput Virtual Screening Identifies Novel N’-(1-Phenylethylidene)-benzohydrazides as Potent, Specific, and Reversible LSD1 Inhibitors; J. Med. Chem. 56 9496 2) Hosseini and Minucci (2017) A comprehensive review of lysine-specific demethylase 1 and its roles in cancer; Epigenomics 9 1123 3) Fiskus et al. (2014), Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells; Leukemia 28 2155 4) Wen et al. (2018), Novel combination of histone methylation modulators with therapeutic synergy against acute myeloid leukemia in vitro and in vivo; Cancer Lett. 413 35 5) Tsai et al. (2018), Stress-induced phosphoprotein 1 acts as a scaffold protein for glycogen synthase kinase-3 beta-mediated phosphorylation of lysine-specific demethylase 1; Oncogenesis 7 31 6) Lu et al. (2018), Hypoxia Promotes Resistance to EGFR Inhibition in NSCLC Cells via the Histone Demethylases LSD1 and PLU-1; Mol. Cancer Epub ahead of print June 22, 2018 7) Ambrosio et al. (2017), Lysine-specific demethylase LSD1 regulates autophagy in neuroblastoma through SESN2-dependent pathway; Oncogene 36 36701

SP2509 Preparation Products And Raw materials

Raw materials

Preparation Products

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SP2509 Suppliers

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1423715-09-6, SP2509Related Search:

Cantharidin (+)-Camptothecin Brefeldin A Adapalene (+)-JQ1 GSK J4 HCl GSK 343 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol MM-102 Volasertib (BI 6727)

(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide

HCI-2509

(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide SP2509

SP2509

3-(4-Morpholinylsulfonyl)benzoic acid (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide

SP-2509;HCI-2509

SP 2509;SP-2509

CS-1755

SP2509 USP/EP/BP

Benzoic acid, 3-(4-morpholinylsulfonyl)-, (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide

(E)-N'-(1-(5-Chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide

1423715-09-6

Inhibitors