A reversible inhibitor of LSD1
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SP-2509

Item No. 15487

Technical Information
Formal Name
3-(4-morpholinylsulfonyl)-benzoic acid (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide
CAS Number
1423715-09-6
Synonyms
  • HCI-2509
  • LSD1 Inhibitor VII
Molecular Formula
C19H20ClN3O5S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 50 mg/mlDMSO: 25 mg/ml
λmax
220, 284, 336 nm
SMILES
O=S(C1=CC(C(N/N=C(C)/C2=C(O)C=CC(Cl)=C2)=O)=CC=C1)(N3CCOCC3)=O
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+
InChi Key
NKUDGJUBIVEDTF-FYJGNVAPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SP-2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM).1 It has no effect on monoamine oxidases A and B. SP-2509 attenuates the binding of LSD1 to CoREST, allowing increased methylation of H3K4 and driving increased expression of p21, p27, and CCAAT/enhancer binding protein α in cultured acute myeloid leukemia (AML) cells.1,2 It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks.1 Co-treatment of SP2509 with the pan-HDAC inhibitor panobinostat (Item No. 13280) synergistically kills AML cells in vitro and improves survival of mice engrafted with AML cells.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fiskus, W., Sharma, S., Abhyankar, S., et alPre-clinical efficacy of combined therapy with LSD1 antagonist SP-2509 and pan-histone deacetylase inhibitor against AML blast progenitor cells. 1-1.

    2. Fiskus, W., Sharma, S., Shah, B., et alHighly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia 28(11), 2155-2164 (2014).