OTSSP167

Catalog No.S7159 Batch:S715901

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Technical Data

Formula

C25H28Cl2N4O2
Molecular Weight 487.42 CAS No. 1431697-89-0
Solubility (25°C)* In vitro DMSO 2 mg/mL (4.1 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.)

Preparing Stock Solutions

Biological Activity

Description OTSSP167 (OTS167) is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
Targets
MELK [1]
(Cell-free assay)
0.41 nM
In vitro OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, in which MELK is highly expressed, with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which are novel MELK substrates and are important for stem-cell characteristics and invasiveness. OTSSP167 suppresses mammosphere formation of breast cancer cells through the inhibition of PSMA1 phosphorylation. [1]
In vivo OTSSP167 exhibits significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. In MDA-MB-231 model, intravenous administration of OTSSP167 at 20 mg/kg once every two days results in TGI of 73% The oral administration at 10 mg/kg once a day reveals TGI of 72%. OTSSP167 for multiple cancer types in dose-dependent and MELK-dependent manners with no or a little body-weight loss. [1]
Features MELK-selective inhibitor.

Protocol (from reference)

Kinase Assay:[1]
  • in vitro kinase assay

    MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl2, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-32P]ATP for 30 min at 30 °C. The reaction is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation.
Cell Assay:[1]
  • Cell lines

    A549, T47D, DU4475, and 22Rv1, HT1197

  • Concentrations

    0.005-0.1 μM

  • Incubation Time

    72 h

  • Method

    Cell Counting Kit-8
Animal Study:[1]
  • Animal Models

    MDA-MB-231, A549, DU145 xenografts

  • Dosages

    1 mg/kg , 5mg/kg ,10 mg/kg, 20 mg/kg

  • Administration

    oral

Selleck's OTSSP167 has been cited by 16 publications

p53 isoform expression promotes a stemness phenotype and inhibits doxorubicin sensitivity in breast cancer [ Cell Death Dis, 2023, 14(8):509] PubMed: 37553320
p53 isoform expression promotes a stemness phenotype and inhibits doxorubicin sensitivity in breast cancer [ Cell Death Dis, 2023, 14(8):509] PubMed: 37553320
Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent [ Cancers (Basel), 2022, 15(1)208] PubMed: 36612203
Microtubule affinity regulating kinase 4 promoted activation of the NLRP3 inflammasome-mediated pyroptosis in periodontitis [ J Oral Microbiol, 2022, 14(1):2015130] PubMed: 34992737
Wild-type IDH1 inhibits the tumor growth through degrading HIF-α in renal cell carcinoma [ Int J Biol Sci, 2021, 17(5):1250-1262] PubMed: 33867843
MELK promotes Endometrial carcinoma progression via activating mTOR signaling pathway. [ EBioMedicine, 2020, 51:102609] PubMed: 31915116
Kinome expression profiling to target new therapeutic avenues in multiple myeloma. [ Haematologica, 2020, 105(3):784-795] PubMed: 31289205
Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities [ Cell Chem Biol, 2020, 27(10):1285-1295.e4] PubMed: 32783966
Inhibition of MELK produces potential anti-tumour effects in bladder cancer by inducing G1/S cell cycle arrest via the ATM/CHK2/p53 pathway. [ J Cell Mol Med, 2020, 24(2):1804-1821] PubMed: 31821699
Mass Spectrometry-Based Selectivity Profiling Identifies a Highly Selective Inhibitor of the Kinase MELK That Delays Mitotic Entry in Cancer Cells [ J Biol Chem, 2020, 295(8):2359-2374] PubMed: 31896573

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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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