KD 5170 |
Catalog No.GC13435 |
An inhibitor of class I and II HDACs
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 940943-37-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KD 5170 is a novel inhibitor of histone deacetylase with IC50 value of 0.045 μM [1].
Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.
KD 5170 is an inhibitor of histone deacetylase and inhibited recombinant HDAC enzymes with IC50 values of 0.020, 2.0, 0.075, 0.026, 0.014 μM for HADC1, HADC2, HADC3, HADC4 and HADC6, respectively. In HeLa cell, KD5170 resulted in histone hyperacetylation with an EC50 of 25 nM in a concentration-dependent way. In HCT-116 cells, KD 5170 induced p21WAF1 expression and histone H3 and a-tubulin acetylation [1][2]. In both HL-60 leukemia cells and HCT-116 colorectal cancer cells, KD5170 resulted in cell death in a concentration-dependent way [1].
In mice bearing HCT-116 xenograft tumors, KD 5170 significantly inhibited tumor growth [1]. In mice bearing H929 xenograft tumors, KD 5170 decreased tumor volume and significantly prolonged the mean time to endpoint. Also, the increase of histone acetylation was found in spleen and tumor tissues of the mice treated with KD 5170 [3].
References:
[1]. Hassig CA, Symons KT, Guo X, et al. KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther, 2008, 7(5): 1054-1065.
[2]. Payne JE, Bonnefous C, Hassig CA, et al. Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor. Bioorg Med Chem Lett, 2008, 18(23): 6093-6096.
[3]. Feng R, Ma H, Hassig CA, et al. KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling. Mol Cancer Ther, 2008, 7(6): 1494-1505.
Cas No. | 940943-37-3 | SDF | |
Chemical Name | S-(2-(6-(4-(3-(dimethylamino)propoxy)phenylsulfonamido)pyridin-3-yl)-2-oxoethyl) ethanethioate | ||
Canonical SMILES | CN(C)CCCOC1=CC=C(S(NC2=CC=C(C(CSC(C)=O)=O)C=N2)(=O)=O)C=C1 | ||
Formula | C20H25N3O5S2 | M.Wt | 451.56 |
Solubility | ≥ 21.2mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.2145 mL | 11.0727 mL | 22.1455 mL |
5 mM | 0.4429 mL | 2.2145 mL | 4.4291 mL |
10 mM | 0.2215 mL | 1.1073 mL | 2.2145 mL |
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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