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RU-SKI 43, Hhat Inhibitor

RU-SKI 43, Hhat Inhibitor

$139.00
The first potent and specific small molecule inhibitor of Hedgehog acyltransferase (Hhat).
Catalog No. Unit Price Qty
M60100-2s 2 mg solid $139.00

Details

Product Information
Molecular Weight: 388.57
Formula: C22H32N2O2S
Purity: ≥ 98%
CAS#: 1043797-53-0
Solubility: DMSO up to 100 mM
Chemical Name: 2-((2-methylbutyl)amino)-1-(4-((m-tolyloxy)methyl)-3a,4,7,7a-tetrahydrothieno[3,2-c]pyridin-5(6H)-yl)ethanone
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

RU-SKI 43 is the first potent and specific small molecule inhibitor of Hedgehog acyltransferase (Hhat), and directly inhibits palmitoylation of the Shh ligand. It was discovered by a high-throughput screen using a peptide-based assay to monitor Hhat-mediated Shh palmitoylation (IC50 ~0.85 µM). In vitro using purified Hhat and ShhN to analyze the kinetics of compound’s inhibition of ShhN palmitoylation, RU-SKI 43 behaved as an uncompetitive inhibitor (Ki = 7.4 μM) with respect to Shh and as a noncompetitive inhibitor (Ki = 6.9 μM) with respect to [125I]iodo-palmitoyl CoA. In cells, RU-SKI 43 specifically blocks Shh palmitoylation and inhibits autocrine and paracrine Shh signaling. Hhat inhibitor could offer a new treatment modality for cancers characterized by Shh overexpression and extremely poor prognoses.


How to Use:

  • In vitro: RU-SKI 43 was used at 10-20 µM final concentration in vitro and in cellular assays.
  • In vivo: n/a

Reference:

  1. 1. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. (2013) Nat Chem Biol. 9(4):247-9.
  2. 2. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. (2014) Oncogene. In press.




Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 388.57
Formula: C22H32N2O2S
Purity: ≥ 98%
CAS#: 1043797-53-0
Solubility: DMSO up to 100 mM
Chemical Name: 2-((2-methylbutyl)amino)-1-(4-((m-tolyloxy)methyl)-3a,4,7,7a-tetrahydrothieno[3,2-c]pyridin-5(6H)-yl)ethanone
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

RU-SKI 43 is the first potent and specific small molecule inhibitor of Hedgehog acyltransferase (Hhat), and directly inhibits palmitoylation of the Shh ligand. It was discovered by a high-throughput screen using a peptide-based assay to monitor Hhat-mediated Shh palmitoylation (IC50 ~0.85 µM). In vitro using purified Hhat and ShhN to analyze the kinetics of compound’s inhibition of ShhN palmitoylation, RU-SKI 43 behaved as an uncompetitive inhibitor (Ki = 7.4 μM) with respect to Shh and as a noncompetitive inhibitor (Ki = 6.9 μM) with respect to [125I]iodo-palmitoyl CoA. In cells, RU-SKI 43 specifically blocks Shh palmitoylation and inhibits autocrine and paracrine Shh signaling. Hhat inhibitor could offer a new treatment modality for cancers characterized by Shh overexpression and extremely poor prognoses.


How to Use:

  • In vitro: RU-SKI 43 was used at 10-20 µM final concentration in vitro and in cellular assays.
  • In vivo: n/a

Reference:

  1. 1. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. (2013) Nat Chem Biol. 9(4):247-9.
  2. 2. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. (2014) Oncogene. In press.




Products are for research use only. Not for human use.

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