XMD8-92

Catalog No.S7525 Batch:S752501

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Technical Data

Formula

C26H30N6O3
Molecular Weight 474.55 CAS No. 1234480-50-2
Solubility (25°C)* In vitro DMSO 94 mg/mL (198.08 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 XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.
Targets
BMK1 [1]
(Cell-free assay)		 BRD4 (1) [4]
(Cell-free assay)
80 nM(Kd) 170 nM(Kd)
In vitro

XMD8-92, via inhibition of BMK1 activation, significantly induces p21 expression in cells, and mediates suppression of cancer cell proliferation. [1] XMD8-92 markedly abrogates the inhibitive effects of hydroxysafflor yellow A (HSYA) on hepatic stellate cell (HSC) activation, and blockes the HSYA-mediated MEF2C down-regulation. [2]
In vivo

XMD8-92 (50 mg/kg i.p.) significantly inhibit the growth of the xenografted human or syngeneic mouse tumors by blocking tumor cell proliferation and tumor-associated angiogenesis. [1] XMD8-92 inhibits pancreatic tumor xenograft growth by significant downregulation of DCLK1 and several of its downstream targets. [3]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Nod/Scid mice bearing HeLa xenograft, C57Bl/6 mice bearing LL/2 xenograft

  • Dosages

    ~50 mg/kg twice a day

  • Administration

    i.p.

Customer Product Validation

, , Int J Oncol, 2017, 51(1):91-103

Data from [Data independently produced by , , Oncotarget, 2014, 5(10): 3145-58]

Data from [Data independently produced by , , J Cell Physiol, 2014, 229(7): 856-67]

Data from [Data independently produced by , , PLoS One, 2015, 10(4):e0125054]

Selleck's XMD8-92 has been cited by 36 publications

ERK5 promotes autocrine expression to sustain mitogenic balance for cell fate specification in human pluripotent stem cells [ Stem Cell Reports, 2024, S2213-6711(24)00216-9] PubMed: 39151429
GLP-1(7-36) protected against oxidative damage and neuronal apoptosis in the hippocampal CA region after traumatic brain injury by regulating ERK5/CREB [ Mol Biol Rep, 2024, 51(1):313] PubMed: 38374452
Protective effects of macrophage-specific integrin α5 in myocardial infarction are associated with accentuated angiogenesis [ Nat Commun, 2023, 10.1038/s41467-023-43369-x] PubMed: 37985764
Extracellular signal-Regulated Kinase 5 (ERK5) is required for the Yes-associated protein (YAP) co-transcriptional activity [ Cell Death Dis, 2023, 14(1):32] PubMed: 36650140
Extracellular signal-Regulated Kinase 5 (ERK5) is required for the Yes-associated protein (YAP) co-transcriptional activity [ Cell Death Dis, 2023, 14(1):32] PubMed: 36650140
Extracellular signal-Regulated Kinase 5 (ERK5) is required for the Yes-associated protein (YAP) co-transcriptional activity [ Cell Death Dis, 2023, 14(1):32] PubMed: 36650140
Endothelial activation and fibrotic changes are impeded by laminar flow-induced CHK1-SENP2 activity through mechanisms distinct from endothelial-to-mesenchymal cell transition [ Front Cardiovasc Med, 2023, 10:1187490] PubMed: 37711550
Endothelial activation and fibrotic changes are impeded by laminar flow-induced CHK1-SENP2 activity through mechanisms distinct from endothelial-to-mesenchymal cell transition [ Front Cardiovasc Med, 2023, 10:1187490] PubMed: 37711550
Identification of a Novel ERK5 (MAPK7) Inhibitor, MHJ-627, and Verification of Its Potent Anticancer Efficacy in Cervical Cancer HeLa Cells [ Curr Issues Mol Biol, 2023, 45(7):6154-6169] PubMed: 37504304
Glucose Starvation or Pyruvate Dehydrogenase Activation Induce a Broad, ERK5-Mediated, Metabolic Remodeling Leading to Fatty Acid Oxidation [ Cells, 2022, 11(9)1392] PubMed: 35563698

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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.