LMK-235

Name: LMK-235
Brand: Selleck Chemicals
SKU: S7569
Rating: 5 (20 reviews)

For research use only.

Catalog No.S7569

20 publications

CAS No. 1418033-25-6

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

Selleck's LMK-235 has been cited by 20 publications

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Theranostics, 2020, 10(15):6790-6805

PubMed: 32550904 ( click the link to review the publication )

Cancers (Basel), 2020, 10;12(2) pii: E412

PubMed: 32050699 ( click the link to review the publication )

Pathol Res Pract, 2020, 216(4):152867

PubMed: 32067803 ( click the link to review the publication )

Oncogene, 2020, 10.1038/s41388-020-01394-w

PubMed: 32709923 ( click the link to review the publication )

Mol Cell, 2019, 75(4):807-822

PubMed: 31442424 ( click the link to review the publication )

Int J Cancer, 2019, 145(9):2496-2508

PubMed: 30963560 ( click the link to review the publication )

Br J Cancer, 2019, 121(12):1039-1049

PubMed: 31690832 ( click the link to review the publication )

Biochim Biophys Acta Mol Basis Dis, 2019, 1865(6):1701-1712

PubMed: 31002870 ( click the link to review the publication )

Front Cell Neurosci, 2019, 13:468

PubMed: 31708743 ( click the link to review the publication )

Life Sci, 2019, 222:125-132

PubMed: 30851335 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2741

PubMed: 30013077 ( click the link to review the publication )

Clin Epigenetics, 2018, 10(1):120

PubMed: 30257705 ( click the link to review the publication )

Int J Mol Sci, 2018, 19(10)

PubMed: 30321986 ( click the link to review the publication )

Mol Med Rep, 2018, 17(1):1445-1452

PubMed: 29138868 ( click the link to review the publication )

Nat Commun, 2017, 8(1):403

PubMed: 28864822 ( click the link to review the publication )

FEBS J, 2017, 284(23):4035-4050

PubMed: 28985013 ( click the link to review the publication )

J Biol Chem, 2016, 291(14):7386-95

PubMed: 26851285 ( click the link to review the publication )

Oncotarget, 2016, 7(25):37966-37978

PubMed: 27177225 ( click the link to review the publication )

Oncotarget, 2016, 7(39):63829-63838

PubMed: 27564097 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

Targets

HDAC5 ^[1] (Cell-free assay)	HDAC4 ^[1] (Cell-free assay)
4.2 nM	11.9 nM

In vitro

LMK-235 causes HDAC inhibition with IC50 of <1 μM in human cancer cell lines with different sensitivity towards cisplatin. In breast cancer cell line MDA-MB-231, tongue cancer cell line Cal27, and esophagus cell line Kyse510 cell line, LMK-235 displays a high cytotoxicity, and markedly enhances the cytotoxicity of cisplatin. ^[1] In addition, LMK-235 also shows nanomolar activity against multiple malaria parasite life cycle stages. ^[2]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human A2780 cells	MkH5R5l1d3SxeHnjbZR6KGG\|c3H5	MkftO\|IhcA>?	NWW5cZZuS3m2b4TvfIlkcXS7IHHnZYlve3RiY3nzdIxifGmwIILld4l{fGGwdDDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwM{Kg{txO	MmrFNlMzPTJ4MEO=
human A2780 cells	NHTOVmdEgXSxdH;4bYNqfHliYYPzZZk>	MWe3NkBp	MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUCuOFkh\|ryP	M2W1flI{OjV{NkCz
human A2780 cells	MVvDfZRwfG:6aXPpeJkh[XO\|YYm=	MYmxPEBp	NGm4NZFKdmirYnn0bY9vKG:oIFjERWMhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhOThiaILzJIJ6KG[udX;y[ZNk\W6lZTDhd5Nige,:jDDJR\|UxRTBwNkWg{txO	MVSyN\|I2OjZyMx?=
human HepG2 cells	NHr6RpNEgXSxdH;4bYNqfHliYYPzZZk>	Mn[4OFghcA>?	NYrqdphJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzMEBKSzZyPUGuNlYh\|ryP	NXXxUHNmOjR7MES5Olc>
human MDA-MB-231 cells	NHLycZNEgXSxdH;4bYNqfHliYYPzZZk>	MkO1O\|IhcA>?	MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBkcXOybHH0bY4he2Wwc3n0bZZmKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkO3JO69VQ>?	M2LuRVI{OjV{NkCz
human KYSE-510 cells	MV\DfZRwfG:6aXPpeJkh[XO\|YYm=	MWG3NkBp	NW\HW2pQS3m2b4TvfIlkcXS7IHHnZYlve3RiY3nzdIxifGmwIILld4l{fGGwdDDoeY1idiCNWWPFMVUyOCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUKuOFgh\|ryP	NHjtZY0zOzJ3Mk[wNy=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

^[1]

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HDAC IC50 Profiling:

The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company’s standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds.

Cell Research:

^[1]

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Cell lines: A2780, Cal27, Kyse510, and MDA-MB-231 cell lines
Concentrations: ~10 μM
Incubation Time: 72 hours
Method:
The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow MTT to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance s measured at 544 and 690 nm in a FLUOstar microplate reader.

(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	58 mg/mL (197.04 mM)
	Ethanol	58 mg/mL (197.04 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+30%PEG300+5%TW80+ddH2O For best results, use promptly after mixing.	13mg/mL

* 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 Download LMK-235 SDF

Molecular Weight	294.35
Formula	C₁₅H₂₂N₂O₄
CAS No.	1418033-25-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=CC(=CC(=C1)C(=O)NOCCCCCC(=O)NO)C

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

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

HDAC Signaling Pathway Map

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LMK-235