NCD38 

NCD38 is a Lysine-specific demethylase 1 (LSD1) inhibitor with a target IC₅₀ of 0.59 μM. NCD38 selectively disrupts LSD1-GFI1B interactions, dissociates LSD1 and CoREST from the ERG super-enhancer. NCD38 increases apoptosis-related protein levels, induces apoptosis and reduces SOX2 and Oct4 levels. NCD38 can be used for the research of acute myeloid leukemia^[1][2][3].

NCD38 (2 μM; 24 h) selectively disrupts the interaction between GFI1B and the LSD1-CoREST-HDAC1/2 complex in HEL cells^[1].
NCD38 (2 μM; 24 h) induces significant upregulation of ERG transcripts in HEL cells^[1].
NCD38 (2 μM; 48 h) induces ERG protein expression and downregulates the erythroid marker CD235a in HEL cells^[1].
NCD38 (2 μM; 24 h) reduces LSD1 and CoREST occupancy at the ERG super-enhancer in HEL cells^[1].
NCD38 potently and selectively inhibits purified LSD1 protein with an IC₅₀ of 0.59 μM, with no activity against MAO A or MAO B^[2].
NCD38 (0.5-2 μM; 6-9 days) dose-dependently inhibits the proliferation of HEL, CMK11-5, and MDS-L leukemia cells^[2].
NCD38 (2 μM; 48-72 h) induces myeloid differentiation in HEL, CMK11-5, and MDS-L leukemia cells by increasing CD11b expression, decreasing erythroid marker expression, and driving morphologic maturation^[2].
NCD38 (2 μM; 2-6 days) induces G₀/G₁ cell cycle arrest in HEL, CMK11-5, and MDS-L leukemia cells^[2].
NCD38 (2 μM; 48 h) activates myeloid development programs and attenuates oncogenic leukemia stem cell programs in HEL, MDS-L, and CMK11-5 leukemia cells, upregulating 89 common genes including key hematopoietic regulators^[2].
NCD38 (2 μM; 3-48 h) activates the GFI1 super-enhancer within 3 h of treatment in HEL leukemia cells, preceding increases in GFI1 transcript levels (after 12 h) and myeloid differentiation marker CD11b expression (after 24 h)^[2].
NCD38 (2 μM; 48 h)-induced myeloid differentiation in HEL leukemia cells is significantly attenuated in GFI1-knockout sublines^[2].
NCD38 (2-5 μM; 10-14 days) inhibits colony formation and induces myeloid differentiation in primary human AML and MDS leukemia cells, while sparing healthy donor hematopoietic cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NCD38 (20 mg/kg; i.p.; daily; 10 days) achieves long-term survival of NSG mice bearing MDS-related leukemia with complex karyotype and sustains low levels of engrafted human leukemia cells^[2].
NCD38 (repeated 1-week on/off) improves survival in NSG mice bearing MDS-related leukemia with complex karyotype, with 75% of treated mice surviving beyond 4 months^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

566.13

C₃₅H₃₆ClN₃O₂

1456907-39-3

O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N[C@H](C(NCC3=CC(Cl)=CC=C3)=O)CCCCNC4C(C5=CC=CC=C5)C4

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• [1]. Yamamoto R, et al. Selective dissociation between LSD1 and GFI1B by a LSD1 inhibitor NCD38 induces the activation of ERG super-enhancer in erythroleukemia cells. Oncotarget. 2018;9(30):21007-21021. Published 2018 Apr 20.

  [2]. Sugino N, et al. A novel LSD1 inhibitor NCD38 ameliorates MDS-related leukemia with complex karyotype by attenuating leukemia programs via activating super-enhancers. Leukemia. 2017 Nov;31(11):2303-2314.

  [3]. Dai XJ, et al. Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective. J Med Chem. 2020;63(23):14197-14215.  [Content Brief]