BG-45

Research use only, not for human use.

A potent and selective HDAC3 inhibitor with IC50 of 289 nM.

A potent and selective HDAC3 inhibitor with IC50 of 289 nM; shows selectivity over HDAC1 and HDAC2; downregulates phosphorylation (Tyr705 and Ser727) of STAT3 and triggers hyperacetylation of STAT3 in MM cells; significantly enhances bortezomib-induced cytotoxicity; exhibits significant tumor growth inhibition in vivo in a murine xenograft model of human MM.

BG45 (1.875-30 μM; 48 and 72 h) targets multiple myeloma (MM) cells and inhibits cell growth in a dose-dependent manner.BG45 (15 μM; 0-48 h; MM.1S cells) induces apoptosis via caspase-3/PARP cleavage.BG45 (10 and 20 μM; 12 h; MM.1S cells) induces acetylation of histone H2A, H3, and H4 in a dose-dependent manner.BG45 (10 and 20 μM; 10 h; MM.1S cells) induces multiple myeloma (MM) cells toxicity is associated with hyperacetylation of histones and STAT3 and downregulation of p-STAT3.Cell Viability Assay Cell Line:MM.1S, RPMI8226, U266, OPM1, and H929 cells Concentration:1.875, 3.75, 7.5, 15, and 30 μM Incubation Time:48 and 72 hours Result:Inhibited multiple myeloma (MM) cells growth in a dose-dependent manner.Western Blot Analysis Cell Line:MM.1S cells Concentration:15 μM Incubation Time:0, 6, 12, 24, and 48 hours Result:Induced caspase-dependent apoptosis in multiple myeloma (MM) cells.Western Blot Analysis Cell Line:MM.1S cells Concentration:10 and 20 μM Incubation Time:12 hours Result:Increased acetylation of histone in a dose-dependent manner.Western Blot Analysis Cell Line:MM.1S cells Concentration:10 and 20 μM Incubation Time:10 hours Result:Downregulated p-STAT3 in a dose-dependent manner.Increased acetylation of STAT3 in MM.1S cells.

BG45 (15-50 mg/kg; i.p.; 5 days a week for 3 weeks; CB17 SCID mice with MM.1S xenograft model) inhibits human multiple myeloma (MM) cells growth and enhances bortezomib (HY-10227) induced cytotoxicity in vivo. Animal Model:CB17 SCID mice (48-54 days old) with MM.1S xenograft model Dosage:15 and 50 mg/kg Administration:Intraperitoneal injection; 5 days a week for 3 weeks Result:Inhibited MM tumor growth in a dose-dependent fashion.Enhanced either single agent activity in combination with bortezomib (HY-10227).

BG45

Cell Cycle/DNA Damage

HDAC

HDAC1|HDAC2|HDAC3|HDAC6

Cancer

——

926259-99-6

214.2233

C11H10N4O

>98% (HPLC)

DMSO: ≥ 48 mg/mL

O=C(C1=NC=CN=C1)NC2=CC=CC=C2N

2-Pyrazinecarboxamide, N-(2-aminophenyl)-

(-20℃)

With Ice Pack

≥ 2 years