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UNC1999

Cat. No. M3107
UNC1999 Structure
Size Price Availability Quantity
2mg USD 50  USD50 In stock
5mg USD 78  USD78 In stock
10mg USD 120  USD120 In stock
25mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Death Dis (2018). Figure 2. UNC1999
Method western blot
Cell Lines VSMCs
Concentrations 5 μM
Incubation Time 24 h
Results Important to note that UNC1999 stimuli resulted in VSMC numbers visibly reducing as early as 24 h
Protocol (for reference only)
Cell Experiment
Cell lines DLBCL cell line harboring the EZH2Y641N mutant
Preparation method DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentrations of compounds (DMSO control, UNC1999, or UNC2400). The medium which contains the test compound or control is refreshed every 3 days. Using TC20 automated cell counter system to measure the numbers of viable cells from at least three independent experiments . Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 μg of total histones is separated using 15% SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3
Concentrations ~5 μM
Incubation time 8 days
Animal Experiment
Animal models Male Swiss albino mice
Formulation DMSO
Dosages ~150 mg/kg (i.p.), ~50 mg/kg (oral)
Administration Intraperitoneal administration or oral administration
Chemical Information
Molecular Weight 569.74
Formula C33H43N7O2
CAS Number 1431612-23-5
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Qianqian Zhang, et al. MicroRNA-20a Suppresses Tumor Proliferation and Metastasis in Hepatocellular Carcinoma by Directly Targeting EZH1

[2] Chunling Zhou, et al. Development of a UPLC-MS/MS method for determination of a dual EZH1/2 inhibitor UNC1999 in rat plasma

[3] Naoya Mimura. Novel epigenetic therapies for multiple myeloma

[4] Ola Rizq, et al. Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition

[5] Kyle D Konze, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1

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