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UNC1215

Cat. No. M3106
UNC1215 Structure
Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 160  USD160 In stock
50mg USD 595  USD595 In stock
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Quality Control & Documentation
Biological Activity

UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.

Protocol (for reference only)
Cell Experiment
Cell lines HEK293T/17 cells
Preparation method CellTiter-Glo luminescent cell viability assay
Concentrations ~100 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 529.72
Formula C32H43N5O2
CAS Number 1415800-43-9
Solubility (25°C) DMSO ≥ 90 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] Alessandra Feoli, et al. Development of a Microscale Thermophoresis-Based Method for Screening and Characterizing Inhibitors of the Methyl-Lysine Reader Protein MRG15

[2] Qianqian Wang, et al. PHF20L1 antagonizes SOX2 proteolysis triggered by the MLL1/WDR5 complexes

[3] Narkhyun Bae, et al. Developing Spindlin1 small-molecule inhibitors by using protein microarrays

[4] Brandi M Baughman, et al. The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer

[5] Lindsey I James, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

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Keywords: UNC1215 supplier, Epigenetic Reader Domain, inhibitors, activators


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