Tinostamustine(EDO-S101)

Catalog No.S8769

Tinostamustine(EDO-S101) Chemical Structure

Molecular Weight(MW): 415.36

Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).

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Biological Activity

Description Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).
Targets
HDAC6 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
6 nM 9 nM 9 nM 25 nM 72 nM
In vitro

The IC50s of EDO-S101 range between 5-13 μM in 8 myeloma cell lines. EDO-S101 has significant synergistic cytotoxicity with the proteasome inhibitors bortezomib and carfilzomib across all cell types tested. EDO-S101 induces strong protein and histone acetylation and is a strong inducer of pIRE-1, the key activator protein of the UPR in MM cells[2].

Assay
Methods Test Index PMID
Western blot
pATR / pCHK1 / pATM / pCHK2 / p53 / γH2AX; 

PubMed: 28633670     


Dose and time response of different proteins implicated in the DNA damage response pathway analyzed on the MM1S cell line.

Ac-H3 / Ac-H4 / Ac α-tubulin; 

PubMed: 28633670     


Dose response (48 h) of acetylated proteins after EDO-S101 treatment in MM1S, RPMI-8226, and JJN3 cell lines.

caspase-8 / caspase-9 / caspase-7 / caspase-3 / PARP; 

PubMed: 28633670     


Dose and time-response changes of proteins involved in apoptosis after EDO-S101 treatment of MM1S cells.

AIF / COX IV; 

PubMed: 28633670     


Subcellular distribution of AIF in mitochondrial and nuclear fractions, in the MM1S cell line after EDO-S101 treatment.

NOXA / p-MCL1 / p-S-BCL2 / BCL2; 

PubMed: 28753594     


Representative western blots depicting NOXA accumulation and downregulation of BCL2, phospho-BCL2 and phospho-MCL1 and cleavage of PARP.

28633670 28753594
Immunofluorescence
γH2AX / Rad51; 

PubMed: 28633670     


Immunofluorescence assay for γH2AX and RAD51 in JJN3HR cells after 5-h post-irradiation with 2 Gy with or without EDO-S101 treatment. Percentage of foci with double staining for γH2AX and RAD51 are shown on the right side. Data are the mean of three independent experiments. One hundred cells were counted in each experiment.

28633670
Growth inhibition assay
Cell viability; 

PubMed: 28633670     


Seven MM cell lines were incubated with different concentrations of EDO-S101 for 48 h. Cell viability was analyzed by MTT reduction.

28633670

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HL-60 cells
  • Concentrations: 4 μM
  • Incubation Time: 0, 6, 12, 18, 24h
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: subcutaneous Daudi human Burkitt's lymphoma xenograft model
  • Formulation: --
  • Dosages: 39 and 78 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 14 mg/mL (33.7 mM)
Ethanol 2 mg/mL (4.81 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.36
Formula

C19H28Cl2N4O2

CAS No. 1236199-60-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID