Alteminostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Alteminostat 是一种新型组蛋白脱乙酰酶 (HDAC) 抑制剂。

Alteminostat is a novel histone deacetylase (HDAC) inhibitor.

Alteminostat (CKD-581; 1 nM-10 μM; 72 hours) treatment potently reduces cell viability in all four lymphoma cell lines in a concentration-dependent manner. The IC50 values of Alteminostat in SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells are 1.31 nM, 36.91 nM, 1.18 nM, and 31.99 nM, respectively.Alteminostat (CKD-581; 10-300 nM; 24 hours) treatment decreases the expression of BCL-6 as well as BCL-2 in cells.Alteminostat (CKD-581; 30-300 nM; 24 h) treatment results in γH2AX accumulation and PARP1 cleavage in SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells. Alteminostat decreases the protein levels of BCL-XL and MCL-1 in a concentration-dependent manner in OCI-LY1 cells.Alteminostat (CKD-581; 10-300 nM; 6 hours) treatment increases the acetylation of histone H3 in SU-DHL-2 cells. And tubulin acetylation also increased with 10 nM CKD-581. CKD-581 increased the acetylation of target molecules by inhibiting class I-II HDACs in lymphoma cells. Cell Viability Assay Cell Line:SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells.Concentration:1 nM-10 μM Incubation Time:72 hours Result:Potently reduced cell viability in all four lymphoma cell lines in a concentration-dependent manner. Western Blot Analysis Cell Line:SU-DHL-4 and OCI-LY1 cells Concentration:10 nM, 30 nM, 100 nM, 300 nM Incubation Time:24 hours Result:Decreased the expression of BCL-6 as well as BCL-2 in cells.

Alteminostat (CKD-581; 20-40 mg/kg; ntraperitoneal injection; twice a week; for 4 weeks) treatment partially but significantly suppresses tumor growth in SU-DHL-4 xenograft mice. Animal Model:Male NOD.CB17 SCID injected with SU-DHL-4 cells Dosage:20 mg/kg or 40 mg/kg Administration:Intraperitoneal injection; twice a week; for 4 weeks Result:Partially but significantly suppressed tumor growth.

Alteminostat

Cell Cycle/DNA Damage

HDAC

HDAC

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1246374-97-9

492.624

C27H36N6O3

>98% (HPLC)

In Vitro:?DMSO : 230 mg/mL (466.90 mM)

O=C(N1CCN(C)CC1)N(CCCCCCC(NO)=O)C2=CC=C(C3=CC4=C(C=C3)C=NN4C)C=C2

N-[7-(hydroxyamino)-7-oxoheptyl]-4-methyl-N-[4-(1-methyl1H-indazol-6-yl)phenyl]piperazine-1 carboxamide

(-20℃)

With Ice Pack

≥ 2 years