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XMD8-92 ERK inhibitor

Name: XMD8-92
SKU: S7525
Availability: InStock
Rating: 5 (32 reviews)

Cat.No.S7525

XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with K_d of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.

Chemical Structure

Molecular Weight: 474.55

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Ras p38 MAPK Raf JNK MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 KLF TOPK
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Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	474.55	Formula	C₂₆H₃₀N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1234480-50-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (168.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.320mg/ml (2.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 26.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	BMK1 ^[1] (Cell-free assay) 80 nM(Kd) BRD4 (1) ^[4] (Cell-free assay) 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] This compound 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] This compound inhibits pancreatic tumor xenograft growth by significant downregulation of DCLK1 and several of its downstream targets. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/20832753/ [2] https://pubmed.ncbi.nlm.nih.gov/24192313/ [3] https://pubmed.ncbi.nlm.nih.gov/24880079/ [4] https://pubmed.ncbi.nlm.nih.gov/27679845/ [5] https://pubmed.ncbi.nlm.nih.gov/30563338/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p53 BMK1 / p-BMK1		22869143
Immunofluorescence	MDM2		22869143

Tech Support

Handling Instructions

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