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| 25mg |
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Purity: ≥98%
PTACH (also known as NCH-51), a SAHA analog, is a novel and potent inhibitor of human histone deacetylase (HDAC). PTACH exhibits strong growth inhibition against a range of human cancer cell types, with EC50 values between 1 and 10 μM. Histone deacetylase (HDAC) inhibitor NCH-51, PTACH. More successfully than SAHA, NCH-51 could induce apoptosis in a range of lymphoid malignant cell types. NCH-51 increased the protein level of antioxidant molecules such as glutathione S-transferase and peroxiredoxins 1 and 2. By maintaining ROS at a level higher than SAHA, NCH-51 demonstrates cytotoxicity.
| Targets |
HDAC1 ( IC50 = 48 nM ); HDAC4 ( IC50 = 32 nM ); HDAC6 ( IC50 = 41 nM ); HIV-1
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|---|---|
| ln Vitro |
PTACH (compound 51) treatment increases p21WAF1/CIP1 and acetylated histone H4 levels in a dose-dependent manner[1].
PTACH (compound 51) exhibits robust activity in the assay for inhibiting the growth of cancer cells. At EC50 values of 2.3 μM, 9.1 μM, 3.0 μM, 2.6 μM, 1.1 μM, 4.5 μM, 2.4 μM, 5.0 μM, and 4.5 μM for MDA-MB-231, SNB-78, HCT116, NCI-H226, LOX-IMVI, SK-OV-3, RXF-631L, St-4, and DU-145 cells, respectively, PTACH inhibits a variety of cancer cells[1]. PTACH (NCH-51) increases the production of HIV-1 in latently infected OM10.1 cells. This reactivation is linked to a loss of HDAC1 occupancy and subsequent hyperacetylation of histones in nuc-1 at the HIV-1 promoter[2]. |
| Cell Assay |
Cell Line: HCT 116 cells
Concentration: 1 μM, 5 μM, 25 μM Incubation Time: 8 hours Result: Gave rise to elevated and dose-dependent levels of acetylated histone H4 and p21WAF1/CIP1. |
| References |
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| Additional Infomation |
2-methylpropanethioic acid S-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl] ester is an aromatic amide.
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| Molecular Formula |
C20H26N2O2S2
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|---|---|
| Molecular Weight |
390.56264257431
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| Exact Mass |
390.143
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| Elemental Analysis |
C, 61.51; H, 6.71; N, 7.17; O, 8.19; S, 16.42
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| CAS # |
848354-66-5
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| PubChem CID |
11395181
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.588
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| LogP |
5.49
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
26
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C(C)C)SCCCCCCC(NC1SC=C(C2C=CC=CC=2)N=1)=O
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| InChi Key |
MDYDGUOQFUQOGE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H26N2O2S2/c1-15(2)19(24)25-13-9-4-3-8-12-18(23)22-20-21-17(14-26-20)16-10-6-5-7-11-16/h5-7,10-11,14-15H,3-4,8-9,12-13H2,1-2H3,(H,21,22,23)
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| Chemical Name |
S-[7-oxo-7-[(4-phenyl-1,3-thiazol-2-yl)amino]heptyl] 2-methylpropanethioate
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| Synonyms |
NCH-51; NCH 51; NCH51. PTACH
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~128.0 mM）
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 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 25.0 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: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5604 mL | 12.8021 mL | 25.6043 mL | |
| 5 mM | 0.5121 mL | 2.5604 mL | 5.1209 mL | |
| 10 mM | 0.2560 mL | 1.2802 mL | 2.5604 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.
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