| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: =98.77%
LMK-235 (LMK235) is a novel, potent and selective inhibitor of HDAC4 and HDAC5 (histone deacetylase) with potential antitumor activity. Its IC50 values for HDAC4/5 inhibition are 11.9 nM and 4.2 nM, respectively. For HDAC6, HDAC1, HDAC2, HDAC11, and HDAC8, its IC50 values are 55.7 nM, 320 nM, 881 nM, 852 nM, and 1278 nM, in that order. LMK235 demonstrated comparable results to vorinostat in terms of cellular HDAC inhibition in a pan-HDAC assay, but it exhibited more potent cytotoxic effects on the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231. While vorinostat and TSA inhibit HDAC4 and HDAC5 in the higher micromolar range, LMK235 exhibits nanomolar inhibition of these enzymes. Whereas HDAC4 and HDAC5, which are inhibited with low nanomolar IC50 values, are preferred by LMK235, which displayed a novel HDAC isoform selectivity profile in contrast to vorinostat.
| Targets |
HDAC5 ( IC50 = 4.22 nM ); HDAC4 ( IC50 = 11.9 nM ); HDAC6 ( IC50 = 55.7 nM ); HDAC1 ( IC50 = 320 nM ); HDAC11 ( IC50 = 852 nM ); HDAC2 ( IC50 = 881 nM ); HDAC8 ( IC50 = 1278 nM )
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
In accordance with the company's standard operating procedure, the in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) is assessed using a fluorescent-based assay. Using three-fold serial dilution and ten distinct concentrations, starting at 10 μM, the IC50 values are calculated. Vorinostat and TSA are the reference compounds.
|
|
| Cell Assay |
Improved MTT assay is used to determine the rate of cell survival under test substance action. Based on the ability of living cells to convert yellow 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) into violet formazan, which can be measured spectrophotometrically, the assay is implemented. Briefly put, 96-well plates are seeded with 5000, 7000, 8000, and 10,000 cells/well of A2780, Cal27, Kyse510, and MDA-MB-231 cell lines. Cells are exposed to higher concentrations of the test compounds after a 24-hour period. Following a 72-hour incubation period, the addition of MTT solution (5 mg/mL in phosphate buffered saline) is used to assess cell survival. In DMSO, the formazan precipitate dissolves. The absorbance in a FLUOstar microplate reader is measured at 544 and 690 nm[1].
|
|
| Animal Protocol |
C57BL/6-BALB/c mice
20 mg/kg i.p. |
|
| References |
|
| Molecular Formula |
C15H22N2O4
|
|
|---|---|---|
| Molecular Weight |
294.35
|
|
| Exact Mass |
294.16
|
|
| Elemental Analysis |
C, 61.21; H, 7.53; N, 9.52; O, 21.74
|
|
| CAS # |
1418033-25-6
|
|
| Related CAS # |
|
|
| Appearance |
White to off-white solid powder
|
|
| SMILES |
CC1=CC(=CC(=C1)C(=O)NOCCCCCC(=O)NO)C
|
|
| InChi Key |
VRYZCEONIWEUAV-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C15H22N2O4/c1-11-8-12(2)10-13(9-11)15(19)17-21-7-5-3-4-6-14(18)16-20/h8-10,20H,3-7H2,1-2H3,(H,16,18)(H,17,19)
|
|
| Chemical Name |
N-[6-(hydroxyamino)-6-oxohexoxy]-3,5-dimethylbenzamide
|
|
| Synonyms |
LMK 235; LMK235; LMK-235
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 3.0mg/ml (10.19mM) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Hyperacetylation of P. falciparum histones. (Compound 1a is LMK-235)Eur J Med Chem.2014 Jul 23;82:204-13. |
|---|
LMK-235 synergizes with bortezomib in BC cells.Oncotarget.2016 Jun 21;7(25):37966-37978. |
LMK-235 inhibits BC cell proliferation and induces apoptosis.Oncotarget.2016 Jun 21;7(25):37966-37978. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
