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SP2509

Chemical Structure : SP2509

CAS No.: 1423715-09-6

SP2509 (SP-2509)

Catalog No.: PC-43122Not For Human Use, Lab Use Only.

SP2509 is a potent, selective histone demethylase LSD1 (KDM1A) inhibitor with IC50 of 13 nM, shows no activity against MAOA, MAOB, LDH and glucose oxidase.

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Biological Activity

SP2509 is a potent, selective histone demethylase LSD1 (KDM1A) inhibitor with IC50 of 13 nM, shows no activity against MAOA, MAOB, LDH and glucose oxidase.
SP2509 inhibits the colony growth of OCI-AML3 significantly more than of the other AML cell-types, induces more apoptosis of AML cells expressing mutant NPM1 than mixed-lineage leukemia fusion oncoproteins.
SP2509 significantly improves the survival of immune-depleted mice model of AML.
SP2509 is synergistically lethal against cultured and primary AML blasts combined with panobinostat.

Physicochemical Properties

M.Wt 437.8972
Formula C19H20ClN3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 33 mg/mL

Chemical Name/SMILES

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

References

1. Fiskus W, et al. Leukemia. 2014 Nov;28(11):2155-64.

2. Sonnemann J, et al. Br J Haematol. 2017 Dec 3. doi: 10.1111/bjh.14983.

3. Sehrawat A, et al. Proc Natl Acad Sci U S A. 2018 Mar 26. pii: 201719168.

4. Khanal T, et al. Sci Rep. 2017 Sep 6;7(1):10662.

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