Domatinostat (4SC-202)

Catalog No.S7555 Batch:S755502

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Technical Data

Formula

C23H21N5O3S
Molecular Weight 447.51 CAS No. 910462-43-0
Solubility (25°C)* In vitro DMSO 89 mg/mL (198.87 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
Targets
HDAC3 [1]
(Cell-free assay)		 HDAC2 [1]
(Cell-free assay)		 HDAC1 [1]
(Cell-free assay)		 HDAC11 [1]
(Cell-free assay)		 HDAC5 [1]
(Cell-free assay)		 View More
0.57 μM 1.12 μM 1.20 μM 9.7 μM 11.3 μM
In vitro In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1]
In vivo In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. [1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    CRC lines (HT-29, HCT-116, HT-15, and DLD-1)

  • Concentrations

    0.1, 1, 5, 10 μM

  • Incubation Time

    72 hours

  • Method

    CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.
Animal Study:

[1]
  • Animal Models

    A549 NSCLC xenograft model and RKO27 colon carcinoma model

  • Dosages

    120 mg/kg

  • Administration

    p.o.

Selleck's Domatinostat (4SC-202) has been cited by 13 publications

Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051] PubMed: 37598220
Single-cell dissection of Merkel cell carcinoma heterogeneity unveils transcriptomic plasticity and therapeutic vulnerabilities [ Cell Rep Med, 2023, 4(7):101101] PubMed: 37421947
Domatinostat Targets the FOXM1-Survivin Axis to Reduce the Viability of Ovarian Cancer Cells Alone and in Combination with Chemotherapeutic Agents [ Int J Mol Sci, 2023, 24(13)10817] PubMed: 37445993
HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction [ Int J Mol Sci, 2023, 24(7)6228] PubMed: 37047202
Targeting the USP7/RRM2 axis drives senescence and sensitizes melanoma cells to HDAC/LSD1 inhibitors [ Cell Rep, 2022, 40(12):111396] PubMed: 36130505
HDAC Class I Inhibitor Domatinostat Preferentially Targets Glioma Stem Cells over Their Differentiated Progeny [ Int J Mol Sci, 2022, 23(15)8084] PubMed: 35897656
Reduction of Metastasis via Epigenetic Modulation in a Murine Model of Metastatic Triple Negative Breast Cancer (TNBC) [ Cancers (Basel), 2022, 14(7)1753] PubMed: 35406526
4sc-202 and Ink-128 cooperate to reverse the epithelial to mesenchymal transition in OSCC [ Oral Dis, 2021, 10.1111/odi.13860] PubMed: 33772986
Analysis of Dual Class I Histone Deacetylase and Lysine Demethylase Inhibitor Domatinostat (4SC-202) on Growth and Cellular and Genomic Landscape of Atypical Teratoid/Rhabdoid. [ Cancers (Basel), 2020, 23;12(3) pii: E756] PubMed: 32210076

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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