HDAC degrader-2

HDAC degrader-2 (SZ-2) (1-10 μM; 24 h) potently degrades HDAC1 and HDAC2 (with D_max, 24 h values of 99% and 90%, respectively) in MM.1S cells after 24-hour treatment, with minimal effect on other HDAC subtypes at concentrations ≤5 μM^[1].
HDAC degrader-2 (10 μM; 24 h) degrades HDAC1 (with a D_max, 24 h value of 38%) in MCF-7 cells after 24-hour treatment at 10 μM, with no effect on HDAC6^[1].
HDAC degrader-2 (0.016-10 μM; 24 h) induces concentration-dependent degradation of HDAC1 in MM.1S cells after 24-hour treatment, with a DC₅₀, 24 h value of 2.55 μM^[1].
HDAC degrader-2 inhibits purified HDAC1 with an IC₅₀ of 6.41 μM and purified HDAC6 with an IC₅₀ of 0.479 μM, exhibiting preferential potency against HDAC6^[1].
HDAC degrader-2 (5 μM; 24 h) inhibits HDAC6 and class I HDACs in MM.1S cells after 24-hour treatment at 5 μM, as shown by increased levels of acetylated α-tubulin and acetylated histone H3^[1].
HDAC degrader-2 (10 μM; 24 h) induces HDAC1 degradation in MM.1S cells after 24-hour treatment at 10 μM in a DDB1-dependent manner, as confirmed by lack of activity with the non-DDB1-binding analog SZ-2-N^[1].
HDAC degrader-2 potently inhibits proliferation of MM.1S cells with an IC₅₀ of 3.28 μM and MCF-7 cells with an IC₅₀ of 3.46 μM^[1].
HDAC degrader-2 (SZ-2) (5 μM; 48 h) induces significant apoptosis in MM.1S cells after 48-hour treatment at 5 μM, with activity comparable to the control agent Ricolinostat (HY-16026)^[1].

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