HDAC-IN-101 

HDAC-IN-101 (compound H6M) is a HDAC1 inhibitor and NTR/pH-activated fluorescent inducer, with an IC₅₀ of 65 nM against human HDAC1. HDAC-IN-101 blocks cancer cell proliferation by inhibiting HDAC1. HDAC-IN-101 is reduced by overexpressed nitroreductase to generate H6AQ, a product that emits fluorescence under low pH conditions. HDAC-IN-101 is applicable for cancer-related research^[1].

HDAC-IN-101 (compound H6M) potently inhibits purified HDAC1 enzyme with an IC₅₀ of 65 nM^[1].
HDAC-IN-101 (H6M) (72 h) inhibits the proliferation of HeLa, HepG2, HCT116, and H1299 cancer cells with IC₅₀ values of 3.59, 3.55, 3.23, and 2.57 μM, respectively, and shows lower cytotoxicity to normal LO2 cells with an IC₅₀ of 12.98 μM following 72 h of incubation^[1].
HDAC-IN-101 (H6M) (5 μM) is pH independent, displaying minimal fluorescence intensity across pH 4.33 to 7.40 at a concentration of 5 μM when excited at 450 nm^[1].
HDAC-IN-101 (H6M) (5 μM; 0-6 h) is activated by 10 μg/mL NTR and 500 μM NADH at pH 4.00, showing time-dependent fluorescence enhancement at 500 nm over 6 h of incubation^[1].
HDAC-IN-101 (H6M) (5 μM) shows high selectivity for NTR and low pH (4.00), exhibiting significant fluorescence enhancement at 500 nm only when treated with 10 μg/mL NTR and 500 μM NADH at pH 4.00^[1].
HDAC-IN-101 (H6M) (1 μM; 0-4 h) selectively activates fluorescence in HeLa cells with high NTR expression, showing time-dependent enhancement over 4 h of incubation, while displaying minimal fluorescence in LO2 cells^[1].

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

HDAC-IN-101 (compound H6M) (40 mg/kg; i.v.; single dose) produces a tumor-specific fluorescence signal with a tumor-to-normal tissue ratio of 3.17 to 12.09, enabling accurate tumor margin identification and imaging-guided resection in HeLa xenograft-bearing BALB/c nude mice^[1].

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

453.45

C₂₅H₁₉N₅O₄

1616863-09-2

O=C(C1=CC=C(C=C1)CNC2=CC3=C(C(C4=CC=C(C=C4)[N+]([O-])=O)=N2)NC5=C3C=CC=C5)NO

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Luo J, et al. A "Double-Locked" and Enzyme/pH-Activated Theranostic Agent for Accurate Tumor Imaging and Therapy. Molecules. 2022;27(2):425. Published 2022 Jan 10.  [Content Brief]