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T2AA 

Cat. No. M28293
T2AA  Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 170  USD170 In stock
25mg USD 350  USD350 In stock
50mg USD 550  USD550 In stock
100mg USD 850  USD850 In stock
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Quality Control & Documentation
Biological Activity

T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase.

Chemical Information
Molecular Weight 511.09
Formula C15H15I2NO3
CAS Number 1380782-27-3
Form Solid
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] André van Helvoort Lengert, et al. Front Biosci (Landmark Ed). Potential New Therapeutic Approaches for Cisplatin-Resistant Testicular Germ Cell Tumors

[2] Delphine Ohayon, et al. J Exp Med. Cytosolic PCNA interacts with p47phox and controls NADPH oxidase NOX2 activation in neutrophils

[3] Rosemary H C Wilson, et al. DNA Repair (Amst). PCNA dependent cellular activities tolerate dramatic perturbations in PCNA client interactions

[4] Akira Inoue, et al. J Biol Chem. A small molecule inhibitor of monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA) inhibits repair of interstrand DNA cross-link, enhances DNA double strand break, and sensitizes cancer cells to cisplatin

[5] Chandanamali Punchihewa, et al. J Biol Chem. Identification of small molecule proliferating cell nuclear antigen (PCNA) inhibitor that disrupts interactions with PIP-box proteins and inhibits DNA replication

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Keywords: T2AA  supplier, DNA/RNA Synthesis, inhibitors, activators


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