1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. HDAC
    Apoptosis
  3. Alteminostat

Alteminostat (Synonyms: CKD-581)

Cat. No.: HY-109109
Handling Instructions

Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research.

For research use only. We do not sell to patients.

Alteminostat Chemical Structure

Alteminostat Chemical Structure

CAS No. : 1246374-97-9

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Description

Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research[1].

In Vitro

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[1].
Alteminostat (CKD-581; 10-300 nM; 24 hours) treatment decreases the expression of BCL-6 as well as BCL-2 in cells[1].
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[1].
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[1].

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

Cell Viability Assay[1]

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[1]

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.
In Vivo

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[1].

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

Animal Model: Male NOD.CB17 SCID injected with SU-DHL-4 cells[1]
Dosage: 20 mg/kg or 40 mg/kg
Administration: Intraperitoneal injection; twice a week; for 4 weeks
Result: Partially but significantly suppressed tumor growth.
Molecular Weight

492.61

Formula

C₂₇H₃₆N₆O₃

CAS No.

1246374-97-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

AlteminostatCKD-581CKD581CKD 581HDACApoptosisHistone deacetylasesLymphomamyelomaanticancerγH2AXacetylationPARP1apoptosisBCL-2BCL-6BCL-XLInhibitorinhibitorinhibit

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