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Santacruzamate A

Cat. No. M5199
Santacruzamate A Structure
Synonym:

CAY10683

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 65  USD65 In stock
50mg USD 250  USD250 In stock
100mg USD 375  USD375 In stock
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Biological Activity

Santacruzamate A is a potent and selective histone deacetylase inhibitor. Santacruzamate A (1), which has several structural features in common with suberoylanilide hydroxamic acid [(2), SAHA, trade name Vorinostat], a clinically approved histone deacetylase (HDAC) inhibitor used to treat refractory cutaneous T-cell lymphoma. Recognition of the structural similarly of 1 and SAHA led to the characterization of santacruzamate A as a picomolar level selective inhibitor of HDAC2, a Class I HDAC, with relatively little inhibition of HDAC4 or HDAC6, both Class II HDACs. As a result, chemical syntheses of santacruzamate A as well as a structurally intriguing hybrid molecule, which blends aspects of both agents (1 and 2), were achieved and evaluated for their HDAC activity and specificity.

Product Citations
Chemical Information
Molecular Weight 278.35
Formula C15H22N2O3
CAS Number 1477949-42-0
Solubility (25°C) DMSO 10 mM
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] Lin Zhang, et al. Santacruzamate A Compositions, Analogs and Methods of Use: A Patent Evaluation of WO 2014/018913 (A2)

[2] Lei Chen, et al. Santacruzamate A Ameliorates AD-Like Pathology by Enhancing ER Stress Tolerance Through Regulating the Functions of KDELR and Mia40-ALR in vivo and in vitro

[3] Rosario Randino, et al. Synthesis and biological evaluation of Santacruzamate-A based analogues

[4] Samantha M Gromek, et al. Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity

[5] Christopher M Pavlik, et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp

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Keywords: Santacruzamate A, CAY10683 supplier, HDAC, inhibitors, activators


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