RUSKI-43 HCl | CAS#1782573-67-4

MedKoo Cat#: 555666 | Name: RUSKI-43 HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

RUSKI 43 is an inhibitor of Hat. It blocks palmitoylation of Shh without affecting palmitoylation of H-Ras or Fyn, myristoylation of c-Src, or acylation of Wnt3a. RU-SKI-43 reduced pancreatic cancer cell proliferation and Gli-1 activation through Smoothened-independent non-canonical signaling. In addition, RU-SKI 43 treatment inhibited two key proliferative pathways regulated by Akt and mTOR.

Chemical Structure

RUSKI-43 HCl

CAS#1782573-67-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 555666

Name: RUSKI-43 HCl

CAS#: 1782573-67-4 (HCl)

Chemical Formula: C22H31ClN2O2S

Exact Mass: 0.0000

Molecular Weight: 423.01

Elemental Analysis: C, 62.47; H, 7.39; Cl, 8.38; N, 6.62; O, 7.56; S, 7.58

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 400.00
10mg	USD 650.00

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Related CAS #

1043797-53-0 (free base) 1782573-67-4 (HCl)

Synonym

RU-SKI43 HCl; RU-SKI43 hydrochloride; RU-SKI 43; RU-SKI-43; RU-SKI43; RUSKI 43; RUSKI-43; RUSKI43;

IUPAC/Chemical Name

1-[6,7-dihydro-4-[(3-methylphenoxy)methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-ethanone, monohydrochloride

InChi Key

JBBKLHJLHRGJSQ-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H30N2O2S.ClH/c1-4-16(2)13-23-14-22(25)24-10-8-21-19(9-11-27-21)20(24)15-26-18-7-5-6-17(3)12-18;/h5-7,9,11-12,16,20,23H,4,8,10,13-15H2,1-3H3;1H

SMILES Code

CCC(C)CNCC(N1CCC2=C(C=CS2)C1COC3=CC=CC(C)=C3)=O.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, DMF, and ethanol

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

RUSKI-43 is an inhibitor of Hhat (IC50 = 0.85 µM). It blocks palmitoylation of Shh without affecting palmitoylation of H-Ras or Fyn, myristoylation of c-Src, or acylation of Wnt3a. In pancreatic cancer cells, RUSKI-43 reduces both Gli1 activation and proliferation. In vitro activity In vivo activity

In vitro activity:

RUSKI-43 was shown to possess cytotoxic activity unrelated to canonical Shh signaling. This study found that RUSKI-43 exhibits off-target cytotoxicity, masking its effect on Hhat-dependent signaling, meaning results obtained with this compound in cells should be treated with caution. Reference: ACS Chem Biol. 2016 Dec 16;11(12):3256-3262. https://pubmed.ncbi.nlm.nih.gov/27779865/

In vivo activity:

To be determined

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	70.92
	DMSO	30.0	70.92
	Ethanol	30.0	70.92

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 423.01 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Rodgers UR, Lanyon-Hogg T, Masumoto N, Ritzefeld M, Burke R, Blagg J, Magee AI, Tate EW. Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. ACS Chem Biol. 2016 Dec 16;11(12):3256-3262. doi: 10.1021/acschembio.6b00896. Epub 2016 Oct 25. PMID: 27779865; PMCID: PMC5349656.

In vitro protocol:

In vivo protocol:

To be determined

1: Jin X, Wang J, Li Q, Zhuang H, Yang J, Lin Z, Lin T, Lv Z, Shen L, Yan C, Zheng J, Zhu J, Gong Z, Wang C, Gao K. SPOP targets oncogenic protein ZBTB3 for destruction to suppress endometrial cancer. Am J Cancer Res. 2019 Dec 1;9(12):2797-2812. Erratum in: Am J Cancer Res. 2021 Apr 15;11(4):1792-1794. Erratum in: Am J Cancer Res. 2023 Nov 15;13(11):5748-5749. PMID: 31911863; PMCID: PMC6943363. 2: Rodgers UR, Lanyon-Hogg T, Masumoto N, Ritzefeld M, Burke R, Blagg J, Magee AI, Tate EW. Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. ACS Chem Biol. 2016 Dec 16;11(12):3256-3262. doi: 10.1021/acschembio.6b00896. Epub 2016 Oct 25. PMID: 27779865; PMCID: PMC5349656.