Description:
YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 inhibitor 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 inhibitor 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 inhibitor 40 (2.5-10 uM) induces apoptosis in THP-1 cell line after 24 h treatment.YTHDC1 inhibitor 40 is a tool compound for studying the role of YTHDC1 in AML.
Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance,
we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one
month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at
least 1 hour.
Reference:
[1]. František Zálešák, et al. Structure-Based Design of a Potent and Selective YTHDC1 Ligand. J Med Chem. 2024 Jun 13;67(11):9516-9535.