1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. CAY10566

CAY10566 

Cat. No.: HY-15823 Purity: 99.01%
Handling Instructions

CAY10566 is a stearoyl-CoA desaturase (SCD) inhibitor.

For research use only. We do not sell to patients.

CAY10566 Chemical Structure

CAY10566 Chemical Structure

CAS No. : 944808-88-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 163 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 290 In-stock
Estimated Time of Arrival: December 31
25 mg USD 590 In-stock
Estimated Time of Arrival: December 31
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Description

CAY10566 is a stearoyl-CoA desaturase (SCD) inhibitor.

IC50 & Target

SCD[1]

In Vitro

Treatment with specific SCD inhibitor CAY10566 dose-dependently reduces SCD activity in MOVAS-1 cells resulting in a significant increase in endoplasmic reticulum (ER) stearate levels. SCD inhibition by CAY10566 treatment induces mineralization and osteoblastic differentiation of MOVAS-1 cells. Along with induction of vascular calcification, CAY10566 dose-dependently induces total ATF4, p-ATF4, and p-eIF2α protein expression. ATF4 mRNA, CHOP protein, CHOP mRNA, and sXBP-1 mRNA levels are also highly and dose-dependently induced by CAY10566 treatment. Phosphorylated PKR-like endoplasmic reticulum kinase (PERK) levels are increased by 15.7-fold at 2 h of CAY10566 treatment, whereas p-eIF2α levels are transiently increased by 1.91-fold at 6 h of CAY10566 treatment. The expressions of ATF4, CHOP, and sXBP mRNA are induced up to 96 h of 300 nM CAY10566 treatment[1].

In Vivo

After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[2].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8 mg/mL (20.52 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5654 mL 12.8268 mL 25.6535 mL
5 mM 0.5131 mL 2.5654 mL 5.1307 mL
10 mM 0.2565 mL 1.2827 mL 2.5654 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

MOVAS-1 cells treated with CAY10566 are incubated with 200 μM stearate-BSA complex containing 1 μCi 14C-stearate. Total lipids are saponified with 3 M sodium hydroxide/ethanol. The saponified fatty acids are separated by 10% silver nitrate-coated thin-layer chromatography. The ratio of the cpm in the band corresponding to oleic acid to the cpm in the band corresponding to stearate is used to calculate stearoyl-CoA desaturase (SCD) activity as previously described[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

To generate allografts, 1×107 immortalized baby mouse kidney (iBMK) cells are implanted in Matrigel into nu/nu athymic female mice. After establishment of palpable tumors, mice are randomized to receive 2.5 mg/kg CAY10566 orally twice daily in 0.5% methylcellulose or vehicle control. Xenograft tumors are measured biweekly and tumor volume calculated as volume=(length×width2×π)/6[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

389.81

Formula

C₁₈H₁₇ClFN₅O₂

CAS No.

944808-88-2

SMILES

CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CAY10566
Cat. No.:
HY-15823
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CAY10566

Cat. No.: HY-15823