2411379-14-9
2411379-14-9 structure
- Name: HDAC/Top-IN-1
- Chemical Name: HDAC/Top-IN-1
- CAS Number: 2411379-14-9
- Molecular Formula: C29H25FN4O4
- Molecular Weight: 512.53
- Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
- Create Date: 2022-06-03 11:38:07
- Modify Date: 2025-08-26 11:48:51
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HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1].
| Name | HDAC/Top-IN-1 |
|---|
| Description | HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1]. |
|---|---|
| Related Catalog | |
| Target |
HDAC1:34 nM (IC50) HDAC2:140 nM (IC50) HDAC3:59 nM (IC50) HDAC6:89 nM (IC50) HDAC8:9.8 μM (IC50) |
| In Vitro | HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines[1]. HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells[1]. HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner[1]. HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase[1]. Cell Proliferation Assay Cell Line: MCF-7, A549, HCT116, HepG-2, K562 and HEL[1] Concentration: 0-2 μM Incubation Time: 48 hours Result: Exhibited remarkable inhibitory activities against the tested cell lines, and IC50s of 0.68, 0.21, 0.26, 0.35 and 0.029 μM in MCF-7, A549, HCT116, HepG-2, K562 and HEL, respectively. Western Blot Analysis Cell Line: HEL[1] Concentration: 20 and 100 nM Incubation Time: 24 hours Result: Dramatically increased in acetyl-H3 and acetyl-H4 levels. Apoptosis Analysis Cell Line: HEL[1] Concentration: 0.1 and 0.5 μM Incubation Time: 48 hours Result: Led to 56.02% and 76.45% apoptotic cell death at concentration of 0.1 and 0.5 μM, respectively Cell Cycle Analysis Cell Line: HEL[1] Concentration: 0.02, 0.1 and 0.5 μM Incubation Time: 48 hours Result: The ratios in the S phase were changed dramatically 9.8%, 15.4%, and 25.8% at 0.02, 0.1 and 0.5 μM, respectively. |
| In Vivo | HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg[1]. HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity[1]. Animal Model: Female BALB/C nude mice (5-6 weeks, 18-20 g; injected with human K562 cells)[1] Dosage: 5 and 10 mg/kg Administration: PO; daily, for 14 days Result: Exhibited potent oral antitumor activity at 5 mg/kg with a TGI value of 41.4% and a T/C value of 54.3%, and achieved better tumor growth inhibition with a TGI of 68.5% and a T/C of 25.5%. |
| References |
| Molecular Formula | C29H25FN4O4 |
|---|---|
| Molecular Weight | 512.53 |