KG-501

Catalog No.S8409 Batch:S840901

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Technical Data

Formula

C17H13ClNO5P
Molecular Weight 377.72 CAS No. 18228-17-6
Solubility (25°C)* In vitro DMSO 20 mg/mL (52.94 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 KG-501 is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
Targets
CREB [1]
In vitro

KG-501 inhibits induction of cAMP-responsive genes, at least in part, by blocking the CREB:CBP interaction[1]. The inhibition of the CREB pathway using KG-501, induces an inhibition of neurite outgrowth and synaptogenesis, as well as a decrease of MAP2+ neuronal cells[2].
In vivo

KG-501 inhibits CREB, CCL2 expression and ERK phosphorylation, also significantly lowers the cAMP level. CREB might contribute to the neuroprotection opposed neuroinflammation through cAMP/ERK adjustment pathway. KG-501 significantly promots the neurological outcomes of AOM-treated mice, reduces phosphorylation of ERK and the concentration of cAMP in cortex[3].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HEK293T cells

  • Concentrations

    5, 10, 25 μM

  • Incubation Time

    20 min

  • Method

    EVX-1 luciferase reporter plasmid was transfected into HEK293T cells. At 24 h posttransfection, cells were pretreated with the indicated amount of KG-501 or DMSO vehicle for 20 min followed by coincubation with forskolin or DMSO. Cells were harvested at 4 h, and luciferase activity was measured.
Animal Study:

[3]
  • Animal Models

    Murine azoxymethane (AOM) model of hepatic encephalopathy (Adult male C57BL/6 mice)

  • Dosages

    10, 20, or 50 μM

  • Administration

    intracerebroventricular infusion

Selleck's KG-501 has been cited by 16 publications

LIM1 contributes to the malignant potential of endometrial cancer [ Front Oncol, 2023, 13:1082441] PubMed: 36969081
Sirt3 mediates the benefits of exercise on bone in aged mice [ Cell Death Differ, 2022, 10.1038/s41418-022-01053-5] PubMed: 36153410
Targeting ADRB2 enhances sensitivity of non-small cell lung cancer to VEGFR2 tyrosine kinase inhibitors [ Cell Death Discov, 2022, 8(1):36] PubMed: 35075132
The chemerin-CMKLR1 axis limits thermogenesis by controlling a beige adipocyte/IL-33/type 2 innate immunity circuit [ Sci Immunol, 2021, 6(61)eabg9698] PubMed: 34330814
Conjugated secondary 12α-hydroxylated bile acids promote liver fibrogenesis [ EBioMedicine, 2021, 66:103290] PubMed: 33752128
FKBP10 promotes proliferation of glioma cells via activating AKT-CREB-PCNA axis [ J Biomed Sci, 2021, 28(1):13] PubMed: 33557829
Long non-coding RNA Lnc-408 promotes invasion and metastasis of breast cancer cell by regulating LIMK1 [ Oncogene, 2021, 10.1038/s41388-021-01845-y] PubMed: 34079084
Recombinant Annexin A2 Administration Improves Neurological Outcomes After Traumatic Brain Injury in Mice [ Front Pharmacol, 2021, 12:708469] PubMed: 34400908
Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling [ Nat Commun, 2020, 11(1):5133] PubMed: 33046706
Cynandione A Alleviates Neuropathic Pain Through α7-nAChR-Dependent IL-10/β-Endorphin Signaling Complexes [ Front Pharmacol, 2020, 11:614450] PubMed: 33584292

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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.