Home MAPK ERK inhibitor - Epigenetic Reader Domain inhibitor XMD8-92 For research use only.

XMD8-92

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

XMD8-92 Chemical Structure

CAS No. 1234480-50-2

Purity & Quality Control

XMD8-92 Related Products

Signaling Pathway

ERK Signaling Pathways

ERK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Function assay Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis, IC50=0.24 μM 21412406
Click to View More Cell Line Experimental Data

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p53 BMK1 / p-BMK1 22869143
Immunofluorescence MDM2 22869143
In Vivo
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]
Animal Research 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.

Chemical Information & Solubility

Molecular Weight 474.55 Formula

C26H30N6O3
CAS No. 1234480-50-2 SDF Download XMD8-92 SDF
Smiles CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (168.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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