UNC 2400 |
| Catalog No.GC15652 |
UNC 2400은 세포 기반 연구에 대한 음성 대조군으로서 UNC1999보다 1,000배 이상 낮은 효능을 가진 UNC1999와 유사한 유사체입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1433200-49-7
Sample solution is provided at 25 µL, 10mM.
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UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1 [1].
Histone-lysine N-methyltransferase (EZH1 or EZH2) is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a transcriptionally repressive post-translational modification. Hypertrimethylation of H3K27 and overexpression of EZH2 are involved in cancers [1].
UNC 2400 is a negative control of UNC1999. UNC 2400 inhibited EZH2 with IC50 value of 13 µM and exhibited >1,000-fold less potency than UNC1999. Also, UNC 2400 inhibited EZH1 and EZH2 Y641F with IC50 values of 62 and >200 µM, respectively. In MCF10A cells, UNC 2400 exhibited little inhibition of H3K27me3 levels and had low cellular toxicity with EC50 value of 27.5 µM that was similar to UNC1999. In DB cells, UNC 2400 (3 µM) did not significantly inhibit DB cell proliferation and had no influence on H3K27me3 or EZH2 levels [1].
Reference:
[1]. Konze KD, Ma A, Li F, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol, 2013, 8(6): 1324-1334.
| Cas No. | 1433200-49-7 | SDF | |
| Chemical Name | N-((1,6-dimethyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-methyl-1H-indazole-4-carboxamide | ||
| Canonical SMILES | CC(C)N1CCN(C2=NC=C(C3=CC(N(C(C)C)N=C4)=C4C(C(N(C)CC5=C(CCC)C=C(C)N(C)C5=O)=O)=C3)C=C2)CC1 | ||
| Formula | C35H47N7O2 | M.Wt | 597.79 |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl | 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. |
||
| 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 | 1.6728 mL | 8.3641 mL | 16.7283 mL |
| 5 mM | 0.3346 mL | 1.6728 mL | 3.3457 mL |
| 10 mM | 0.1673 mL | 0.8364 mL | 1.6728 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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.
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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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