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SGC-CBP30

Cat. No. M9141
SGC-CBP30 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 170  USD170 In stock
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
25mg USD 280  USD280 In stock
50mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

Sgc-cbp30 is a potent and highly selective CBP/ P300 bromine domain inhibitor (Kd of 21 nM and 32 nM against CBP and P300, respectively), which is 40 times more selective than BRD4 [BRD4(1)]. Sgc-cbp30 strongly reduces the secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

Chemical Information
Molecular Weight 509.04
Formula C28H33ClN4O3
CAS Number 1613695-14-9
Solubility (25°C) DMSO: ≥ 30 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] Tao J, et al. Biomed Pharmacother. Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo.

[2] Chua MJ, et al. Int J Parasitol Drugs Drug Resist. Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites.

[3] Xiang Q, et al. Eur J Med Chem. Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.

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