Home Epigenetics HDAC inhibitor Tinostamustine(EDO-S101) For research use only.

Tinostamustine(EDO-S101)

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).

Tinostamustine(EDO-S101) Chemical Structure

Tinostamustine(EDO-S101) Chemical Structure

CAS: 1236199-60-2

Purity & Quality Control

Batch: S876901 DMSO] 14 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.7%
99.7

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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)		 Click to View More Targets
6 nM 9 nM 9 nM 25 nM 72 nM
In vitro
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].
Cell Research Cell lines HL-60 cells
Concentrations 4 μM
Incubation Time 0, 6, 12, 18, 24h
Method

--
Experimental Result Images Methods Biomarkers Images PMID
Western blot pATR / pCHK1 / pATM / pCHK2 / p53 / γH2AX Ac-H3 / Ac-H4 / Ac α-tubulin caspase-8 / caspase-9 / caspase-7 / caspase-3 / PARP AIF / COX IV NOXA / p-MCL1 / p-S-BCL2 / BCL2 28633670
Immunofluorescence γH2AX / Rad51 28633670
Growth inhibition assay Cell viability 28633670
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03903458 Recruiting
Malignant Melanoma
Markus Joerger|Cantonal Hospital of St. Gallen
 March 7 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 415.36 Formula

C19H28Cl2N4O2
CAS No. 1236199-60-2 SDF --
Smiles CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCCCCC(=O)NO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 14 mg/mL ( (33.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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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