LMK-235

Name: LMK-235
Brand: MedChemExpress
SKU: HY-18998
Rating: 5.0 (28 reviews)

Cat. No.: HY-18998 Purity: 98.97%: Data Sheet
SDS

COA
Handling Instructions
FAQs
Technical Support

LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC₅₀s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

For research use only. We do not sell to patients.

LMK-235 Chemical Structure

CAS No. : 1418033-25-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

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Customer Review

Based on 28 publication(s) in Google Scholar

25 Publications Citing Use of MCE LMK-235

: LMK-235 purchased from MedChemExpress. Usage Cited in: Life Sci. 2018 Aug 15;207:386-394. [Abstract]; The protein levels of HDAC4, HDAC5, HO-1, histone 3 acetylation, histone 4 acetylation and Smad7 in CCRF-SB cells are detected by Western blot after LMK-235 treatment at 0.25, 0.5, 1, 2 and 4 μM for 24 h. β-Actin is used as internal reference.

: LMK-235 purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834. [Abstract]; OCILY10 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.

: LMK-235 purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834. [Abstract]; OCI-LY3 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.

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View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HDAC5

4.22 nM (IC₅₀)

HDAC4

11.9 nM (IC₅₀)

HDAC6

55.7 nM (IC₅₀)

HDAC1

320 nM (IC₅₀)

HDAC11

852 nM (IC₅₀)

HDAC2

881 nM (IC₅₀)

HDAC8

1278 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.32 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
A2780	IC₅₀	0.32 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay	[PMID: 23252603]
A2780	IC₅₀	0.49 μM Compound: 19i, LMK235	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	[PMID: 23252603]
A2780	IC₅₀	0.65 μM Compound: 19i, LMK235	Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
A2780	IC₅₀	0.97 μM Compound: 5; LMK235	Cytotoxicity against human A2780 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability by MTT assay	[PMID: 31787463]
CAL-27	IC₅₀	0.36 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin resistant human CAL27 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin resistant human CAL27 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
CAL-27	IC₅₀	0.36 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin sensitive human CAL27 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin sensitive human CAL27 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
CAL-27	IC₅₀	0.76 μM Compound: 5; LMK235	Cytotoxicity against human CAL27 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human CAL27 cells assessed as reduction in cell viability by MTT assay	[PMID: 31787463]
CAL-27	IC₅₀	1.03 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin sensitive human CAL27 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin sensitive human CAL27 cells after 72 hrs by MTT assay	[PMID: 23252603]
CAL-27	IC₅₀	1.81 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin resistant human CAL27 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin resistant human CAL27 cells after 72 hrs by MTT assay	[PMID: 23252603]
HepG2	IC₅₀	0.16 μM Compound: 1a, LMK235	Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs	[PMID: 24904967]
HepG2	IC₅₀	1.26 μM Compound: 1a, LMK235	Cytotoxicity against human HepG2 cells after 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs	[PMID: 24904967]
KYSE-510	IC₅₀	0.35 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin resistant human KYSE-510 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin resistant human KYSE-510 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
KYSE-510	IC₅₀	1 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin sensitive human KYSE-510 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin sensitive human KYSE-510 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
KYSE-510	IC₅₀	2.48 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin resistant human KYSE-510 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin resistant human KYSE-510 cells after 72 hrs by MTT assay	[PMID: 23252603]
KYSE-510	IC₅₀	2.96 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin sensitive human KYSE-510 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin sensitive human KYSE-510 cells after 72 hrs by MTT assay	[PMID: 23252603]
MDA-MB-231	IC₅₀	0.41 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin resistant human MDA-MB-231 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin resistant human MDA-MB-231 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
MDA-MB-231	IC₅₀	0.46 μM Compound: 19i, LMK235	Inhibition of HDAC in cisplatin sensitive human MDA-MB-231 cells after 18 hrs by fluorescence assay Inhibition of HDAC in cisplatin sensitive human MDA-MB-231 cells after 18 hrs by fluorescence assay	[PMID: 23252603]
MDA-MB-231	IC₅₀	1.37 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin sensitive human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin sensitive human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 23252603]
MDA-MB-231	IC₅₀	1.68 μM Compound: 19i, LMK235	Cytotoxicity against cisplatin resistant human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against cisplatin resistant human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 23252603]

In Vitro

LMK-235 shows cytotoxic activity against human ovarian cancer cell lines A2780 and A2780 CisR, with IC₅₀s of 0.49 μM and 0.32 μM, respectively. LMK-235 inhibits HDAC in A2780 and A2780 CisR cell lines, with IC₅₀s of 0.65 μM and 0.32 μM, respectively. LMK-235 produces a higher reduction in cell viability in comparison to the combination of cisplatin and vorinostat in all cell lines^[1]. LMK-235 (0, 0.625, 1.25, 2.5, 5, 10, and 20 μM) reduces the proliferation of BC cells in a dose- and time-dependent manner. LMK-235 (0-800 nM) also inhibits the growth of BC cells. Moreover, LMK-235 synergizes with bortezomib in BC cell lines^[2]. LMK235 (2, 20 nM) decreases in HDAC4 nuclear accumulation in Cdkl5 -/Y NPCs, completely restores the reduced number of neurons generated from Cdkl5 -/Y NPCs. LMK235 also restores histone 3 acetylation in Cdkl5 -/Y NPCs. LMK235 causes a notable increase in the isoform IV, but does not affect BDNF isoforms I or II^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LMK235 (5 and 20 mg/kg) restores survival and maturation of postmitotic granule neurons in Cdkl5 -/Y mice. LMK235 also restores synapse development in the dentate gyrus and hippocampus of Cdkl5 -/Y mice. Furthermore, LMK235 restores hippocampus-dependent learning and memory in Cdkl5 -/Y mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

294.35

Formula

C₁₅H₂₂N₂O₄

CAS No.

1418033-25-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(NOCCCCCC(NO)=O)C1=CC(C)=CC(C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (101.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3973 mL	16.9866 mL	33.9732 mL
5 mM	0.6795 mL	3.3973 mL	6.7946 mL
10 mM	0.3397 mL	1.6987 mL	3.3973 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (242 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Marek L, et al. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013 Jan 24;56(2):427-36. [Content Brief]

[2]. Li A, et al. HDAC5, a potential therapeutic target and prognostic biomarker, promotes proliferation, invasion and migration in human breast cancer. Oncotarget. 2016 Jun 21;7(25):37966-37978. [Content Brief]

[3]. Trazzi S, et al. HDAC4: a key factor underlying brain developmental alterations in CDKL5 disorder. Hum Mol Genet. 2016 Sep 15;25(18):3887-3907. [Content Brief]

Cell Assay
^[1]

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 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (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 is measured at 544 and 690 nm in a FLUOstar microplate reader^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Marek L, et al. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013 Jan 24;56(2):427-36. [Content Brief]

[2]. Li A, et al. HDAC5, a potential therapeutic target and prognostic biomarker, promotes proliferation, invasion and migration in human breast cancer. Oncotarget. 2016 Jun 21;7(25):37966-37978. [Content Brief]

[3]. Trazzi S, et al. HDAC4: a key factor underlying brain developmental alterations in CDKL5 disorder. Hum Mol Genet. 2016 Sep 15;25(18):3887-3907. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3973 mL	16.9866 mL	33.9732 mL	84.9329 mL
	5 mM	0.6795 mL	3.3973 mL	6.7946 mL	16.9866 mL
	10 mM	0.3397 mL	1.6987 mL	3.3973 mL	8.4933 mL
	15 mM	0.2265 mL	1.1324 mL	2.2649 mL	5.6622 mL
	20 mM	0.1699 mL	0.8493 mL	1.6987 mL	4.2466 mL
	25 mM	0.1359 mL	0.6795 mL	1.3589 mL	3.3973 mL
	30 mM	0.1132 mL	0.5662 mL	1.1324 mL	2.8311 mL
	40 mM	0.0849 mL	0.4247 mL	0.8493 mL	2.1233 mL
	50 mM	0.0679 mL	0.3397 mL	0.6795 mL	1.6987 mL
	60 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4155 mL
	80 mM	0.0425 mL	0.2123 mL	0.4247 mL	1.0617 mL
	100 mM	0.0340 mL	0.1699 mL	0.3397 mL	0.8493 mL

LMK-235 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LMK-2351418033-25-6LMK235LMK 235HDACHistone deacetylasesInhibitorinhibitorinhibit

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LMK-235

Customer Review

LMK-235 Related Antibodies

25 Publications Citing Use of MCE LMK-235

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Customer Review

LMK-235 Related Antibodies

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Complete Stock Solution Preparation Table

LMK-235 Related Classifications

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