RU-SKI 43

SKU: orb1708617

Description

RU-SKI 43 is a selective hedgehog acyltransferase (Hhat) inhibitor (IC50 = 850 nM) with anticancer properties. It suppresses lung adenocarcinoma cell growth in vitro by inhibiting non-canonical Gli-1 activation and downregulating Akt/mTOR signaling pathways.

Research Area

Metabolism Research, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1043797-53-0
• MW: 386.55
• Purity: 99.92% (May vary between batches)
• Formula: C₂₂H₃₀N₂O₂S
• SMILES: C(OC1=CC(C)=CC=C1)C2C3=C(CCN2C(CNCC(CC)C)=O)SC=C3
• Target: Acyltransferase,Hedgehog/Smoothened

Bioactivity

• Target IC50:
  Hhat:850 nM|[125I]-iodo-palmitoylCoA:6.9 μM(Ki)|Shh:7.4 μM(Ki)
• In Vivo:
  After IV administration,RU-SKI 43 has a t1/2 of 17 min in mouse plasma.
• In Vitro:
  RU-SKI 43 (10 or 20 μM; 5 h; AsPC-1 and Panc-1 pancreatic cancer cells) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours. RU-SKI 43 acts as an uncompetitive inhibitor with a Ki of 7.4 μM concerning Shh, while it functions with a Ki of 6.9 μM regarding 125I-iodo-palmitoylCoA. RU-SKI 43 (10μM; 48 h; AsPC-1 and Panc-1 pancreatic cancer cells) leads to reduced phosphorylation (47-67% decrease) of four proteins within the Akt pathway, which encompass Akt (phosphorylated at Thr307 and Ser473), PRAS40, Bad, and GSK-3β. Additionally, RU-SKI 43 treatment results in decreased phosphorylation of mTOR and S6, both of which are constituents of the mTOR signaling pathway. RU-SKI 43 (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells. RU-SKI 43 (10 μM; for 72 h; AsPC-1 and Panc-1 pancreatic cancer cells) causes a 40% decrease in Gli-1 levels in AsPC-1 cells.

Storage & Handling

• Storage: Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Hhat, Hedgehog, Acyltransferase, RUSKI 43, RU-SKI 43, RUSKI43, RUSKI-43, Smoothened

Compound Identifiers

PubChem CID

46006640