XMD8-92

Catalog No.S7525

For research use only.

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.

XMD8-92 Chemical Structure

CAS No. 1234480-50-2

Selleck's XMD8-92 has been cited by 24 publications

Purity & Quality Control

Choose Selective ERK Inhibitors

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 M{DITGZ2dmO2aX;uJIF{e2G7 MoXJTY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDCUWsyKGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDifUBUTFNvUFHHSUBidmGueYPpd{whUUN3ME2wMlI1KM7:TR?= M1m3fFIyPDF{NEC2
Assay
Methods Test Index PMID
Western blot p53 ; BMK1 / p-BMK1 22869143
Immunofluorescence MDM2 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 (from reference)

Animal Research:

[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 474.55
Formula

C26H30N6O3

CAS No. 1234480-50-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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