XMD8-92

For research use only.

Catalog No.S7525

20 publications

XMD8-92 Chemical Structure

CAS No. 1234480-50-2

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.

Selleck's XMD8-92 has been cited by 20 publications

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Mmi1SpVv[3Srb36gZZN{[Xl? M1vvb2lvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgRm1MOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOgZpkhW0SVLWDBS2Uh[W6jbInzbZMtKEmFNUC9NE4zPCEQvF2= NHTmcGQzOTRzMkSwOi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53; 

PubMed: 22869143     


A549 cells were treated with XMD8-92 (4 μM) for 0, 8, 16, 24, 32 and 40 hours. Cell lysates were analyzed by western blot using anti-p53 or anti-GAPDH antibodies.

BMK1 / p-BMK1 ; 

PubMed: 22869143     


Tumor homogenates from Nod/Scid mice subcutaneously injected with HeLa or A549 cells and treated with control, doxorubicin, XMD8-92 or doxorubicin+XMD8-92 for 30 hr were used in western blot to detect BMK1, p53 and GAPDH expression. n = 3 mice per group. 

22869143
Immunofluorescence
MDM2; 

PubMed: 22869143     


Pml+/+ MEF and Pml−/− MEF cells were treated with XMD8-92 (4 μM) and/or doxorubicin (300 nM) for about 24 hr and stained using anti-PML, anti-MDM2, and anti-Nucleolin antibodies. Arrows indicate translocation of MDM2 to the nucleoli.

22869143
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

Animal Research:

[1]

- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL warmed (153.82 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 474.55
Formula

C26H30N6O3

CAS No. 1234480-50-2
Storage powder
in solvent
Synonyms N/A
Smiles CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID