CID755673

Catalog No.S7188 Batch:S718801

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Technical Data

Formula

C12H11NO3
Molecular Weight 217.22 CAS No. 521937-07-5
Solubility (25°C)* In vitro DMSO 43 mg/mL (197.95 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 CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.
Targets
PKD1 [1] PKD3 [1] PKD2 [1]
180 nM 227 nM 280 nM
In vitro In LNCaP prostate cancer cells, CID755673 directly inhibits PKD1 activity. In HeLa cells, CID755673 significantly blocks PMA-induced nuclear export of HDAC5, and blocks PKD-mediated protein transport. In prostate cancer cells, CID755673 potently blocks cell migration and invasion, and also shows inhibition activity on tumor cell proliferation and cell cycle distribution. [1] In addition, CID755673 alter primary human NK cell effector functions. [3]
In vivo CID755673, via PKD/PKD1 inhibition, significantly ameliorates necrosis and severity of pancreatitis in a rat acute pancreatitis model. [2]

Protocol (from reference)

Kinase Assay: [1]
  • In Vitro Radiometric PKD Kinase Assay

    The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.
Cell Assay:[1]
  • Cell lines

    LNCaP or PC3 cells

  • Concentrations

    ~25 μM

  • Incubation Time

    6 days

  • Method

    Cell proliferation was determined by counting the number of viable cells upon trypan blue staining. Cell proliferation is measured by CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturer's instructions.
Animal Study:[2]
  • Animal Models

    Rat pancreatitis model

  • Dosages

    ~15 mg/kg

  • Administration

    i.p.

Selleck's CID755673 has been cited by 10 publications

Structural insights into regulation of the PEAK3 pseudokinase scaffold by 14-3-3 [ Nat Commun, 2023, 14(1):3543] PubMed: 37336883
Structural insights into regulation of the PEAK3 pseudokinase scaffold by 14-3-3 [ Nat Commun, 2023, 14(1):3543] PubMed: 37336883
FBXO28 suppresses liver cancer invasion and metastasis by promoting PKA-dependent SNAI2 degradation [ Oncogene, 2023, 42(39):2878-2891] PubMed: 37596321
FBXO28 suppresses liver cancer invasion and metastasis by promoting PKA-dependent SNAI2 degradation [ Oncogene, 2023, 10.1038/s41388-023-02809-0] PubMed: 37596321
Chemically induced revitalization of damaged hepatocytes for regenerative liver repair [ iScience, 2023, 26(12):108532] PubMed: 38144457
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710
FBXO22 Possesses Both Protumorigenic and Antimetastatic Roles in Breast Cancer Progression. [ Cancer Res, 2018, 78(18):5274-5286] PubMed: 29945959
Inhibition of protein kinase D disrupts spindle formation and actin assembly during porcine oocyte maturation. [ Aging (Albany NY), 2018, 10(12):3736-3744] PubMed: 30555056
VEGF/PKD-1 signaling mediates arteriogenic gene expression and angiogenic responses in reversible human microvascular endothelial cells with extended lifespan [Best B Mol Cell Biochem, 2018, 446(1-2):199-207] PubMed: 29380239
Klotho suppresses high phosphate-induced osteogenic responses in human aortic valve interstitial cells through inhibition of Sox9. [ J Mol Med (Berl), 2017, 95(7):739-751] PubMed: 28332126

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.