RUSKI-201 HCl | CAS# 2320262-09-5 | Hhat Chemical Probe

MedKoo Cat#: 564615 | Name: RUSKI-201 HCl

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Description:

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

RUSKI-201 is the first selective Hedgehog acyltransferase (Hhat) chemical probe in cells.

Chemical Structure

RUSKI-201 HCl

CAS#2320262-09-5

Theoretical Analysis

MedKoo Cat#: 564615

Name: RUSKI-201 HCl

CAS#: 2320262-09-5

Chemical Formula: C20H29Cl2N3OS

Exact Mass:

Molecular Weight: 430.43

Elemental Analysis: C, 55.81; H, 6.79; Cl, 16.47; N, 9.76; O, 3.72; S, 7.45

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 300.00
5mg	USD 600.00
10mg	USD 900.00

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Synonym

RUSKI201 HCl; RUSKI 201 HCl; RUSKI-201 HCl; RU-SKI-201 HCl; RUSKI201 hydrochloride; RUSKI 201 hydrochloride; RUSKI-201 hydrochloride; RU-SKI-201 hydrochloride;

IUPAC/Chemical Name

2-(2-Methyl-butylamino)-1-[4-(6-methyl-pyridin-2-yl)-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]-ethanone

InChi Key

TUDOZEOETHEGCR-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H27N3OS.2ClH/c1-4-14(2)12-21-13-19(24)23-10-8-18-16(9-11-25-18)20(23)17-7-5-6-15(3)22-17;;/h5-7,9,11,14,20-21H,4,8,10,12-13H2,1-3H3;2*1H

SMILES Code

CCC(C)CNCC(N1CCC2=C(C=CS2)C1C3=NC(C)=CC=C3)=O.Cl.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

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

RU-SKI 201 is an Hhat inhibitor (IC50 = 0.2 μM for recombinant enzyme). It inhibits palmitoylation of sonic hedgehog (Shh) in Shh-overexpressing HEK293 cells with a tagging IC50 (TC50) value of 0.87 μM. RU-SKI 201 inhibits Hh signaling in H520, PANC-1, and MCF-7 cancer cells co-cultured with Shh-Light2 cells (IC50s = 4.8, 7.8, and 8.5 μM, respectively).

In vitro activity:

Unlike RUSKI-43, RUSKI-201 showed no off-target cytotoxicity, and specifically inhibited Hhat in cells. RUSKI-201 is the first selective Hhat chemical probe in cells and should be used in future studies of Hhat catalytic function. 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	69.70
	DMSO	30.0	69.70
	Ethanol	30.0	69.70

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 430.43 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: 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. Epub 2016 Oct 25. PubMed PMID: 27779865; PubMed Central PMCID: PMC5349656.