JW74 | CAS#863405-60-1 | tankyrase inhibitor

JW74
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406500

CAS#: 863405-60-1

Description: JW74 is a tankyrase-specific inhibitor. JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. At the molecular level, JW74 induces stabilization of AXIN2, a key component of the β-catenin destruction complex, resulting in reduced levels of nuclear β-catenin. At the functional level, JW74 induces reduced cell growth in all three tested cell lines, in part due to a delay in cell cycle progression and in part due to an induction of caspase-3-mediated apoptosis. Furthermore, JW74 induces differentiation in U2OS cells, which under standard conditions are resistant to osteogenic differentiation. JW74 also enhances differentiation of OS cell lines, which do not harbor a differentiation block. ( Cancer Med. 2014 Feb;3(1):36-46. )

Chemical Structure

JW74

CAS# 863405-60-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406500
Name: JW74
CAS#: 863405-60-1
Chemical Formula: C24H20N6O2S
Exact Mass: 456.14
Molecular Weight: 456.520
Elemental Analysis: C, 63.14; H, 4.42; N, 18.41; O, 7.01; S, 7.02

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
1g	USD 4350	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: JW74; JW-74; JW 74.

IUPAC/Chemical Name: 5-(((4-(4-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio)methyl)-3-(p-tolyl)-1,2,4-oxadiazole

InChi Key: KRIKILRRJCIWNB-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H20N6O2S/c1-16-3-5-17(6-4-16)22-26-21(32-29-22)15-33-24-28-27-23(18-11-13-25-14-12-18)30(24)19-7-9-20(31-2)10-8-19/h3-14H,15H2,1-2H3

SMILES Code: CC1=CC=C(C2=NOC(CSC3=NN=C(C4=CC=NC=C4)N3C5=CC=C(OC)C=C5)=N2)C=C1

Appearance: white 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, not in water

Shelf Life: >2 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:

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Biological target:	JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
In vitro activity:	In addition, subsequent functional experiments showed that JW74, a specific Wnt/β-catenin signaling inhibitor, inhibited the transcription of LINC01606 and suppressed migration and invasion in GC cell lines. Reference: Int J Biochem Cell Biol. 2018 Oct;103:125-134. https://pubmed.ncbi.nlm.nih.gov/30142387/
In vivo activity:	Long-term treatment with JW74 inhibited the growth of tumor cells in both a mouse xenograft model of CRC and in Apc(Min) mice (multiple intestinal neoplasia, Min). Reference: Cancer Res. 2011 Jan 1;71(1):197-205. https://pubmed.ncbi.nlm.nih.gov/21199802/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	20.0	43.81
	DMF:PBS (pH 7.2) (1:5)	0.2	0.35
	DMSO	38.6	84.44

Preparing Stock Solutions

The following data is based on the product molecular weight 456.52 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. Luo Y, Tan W, Jia W, Liu Z, Ye P, Fu Z, Lu F, Xiang W, Tang L, Yao L, Huang Q, Xiao J. The long non-coding RNA LINC01606 contributes to the metastasis and invasion of human gastric cancer and is associated with Wnt/β-catenin signaling. Int J Biochem Cell Biol. 2018 Oct;103:125-134. doi: 10.1016/j.biocel.2018.08.012. Epub 2018 Aug 22. PMID: 30142387. 2. Gao F, Wang B, Chang T, Li M, Fang W, Li ZH, Gao L. The iron pro-chelator BHAPI attenuates glutamate-induced oxidative stress via Wnt-β/catenin pathway in HT22 cells. Brain Res Bull. 2018 May;139:285-291. doi: 10.1016/j.brainresbull.2018.03.011. Epub 2018 Mar 26. PMID: 29588166. 3. Waaler J, Machon O, von Kries JP, Wilson SR, Lundenes E, Wedlich D, Gradl D, Paulsen JE, Machonova O, Dembinski JL, Dinh H, Krauss S. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. doi: 10.1158/0008-5472.CAN-10-1282. PMID: 21199802.
In vitro protocol:	1. Luo Y, Tan W, Jia W, Liu Z, Ye P, Fu Z, Lu F, Xiang W, Tang L, Yao L, Huang Q, Xiao J. The long non-coding RNA LINC01606 contributes to the metastasis and invasion of human gastric cancer and is associated with Wnt/β-catenin signaling. Int J Biochem Cell Biol. 2018 Oct;103:125-134. doi: 10.1016/j.biocel.2018.08.012. Epub 2018 Aug 22. PMID: 30142387. 2. Gao F, Wang B, Chang T, Li M, Fang W, Li ZH, Gao L. The iron pro-chelator BHAPI attenuates glutamate-induced oxidative stress via Wnt-β/catenin pathway in HT22 cells. Brain Res Bull. 2018 May;139:285-291. doi: 10.1016/j.brainresbull.2018.03.011. Epub 2018 Mar 26. PMID: 29588166.
In vivo protocol:	1. Waaler J, Machon O, von Kries JP, Wilson SR, Lundenes E, Wedlich D, Gradl D, Paulsen JE, Machonova O, Dembinski JL, Dinh H, Krauss S. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. doi: 10.1158/0008-5472.CAN-10-1282. PMID: 21199802.

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1: Liu D, Cui W, Liu B, Hu H, Liu J, Xie R, Yang X, Gu G, Zhang J, Zheng H. Atorvastatin Protects Vascular Smooth Muscle Cells From TGF-β1-Stimulated Calcification by Inducing Autophagy via Suppression of the β-Catenin Pathway. Cell Physiol Biochem. 2014;33(1):129-41. doi: 10.1159/000356656. Epub 2014 Jan 20. PubMed PMID: 24481040.

2: Wessel Stratford E, Daffinrud J, Munthe E, Castro R, Waaler J, Krauss S, Myklebost O. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 2014 Feb;3(1):36-46. doi: 10.1002/cam4.170. Epub 2013 Dec 17. PubMed PMID: 24403055; PubMed Central PMCID: PMC3930388.

3: Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP, Krauss S. Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. J Med Chem. 2013 Apr 11;56(7):3012-23. doi: 10.1021/jm4000566. Epub 2013 Mar 29. PubMed PMID: 23473363.

4: Waaler J, Machon O, von Kries JP, Wilson SR, Lundenes E, Wedlich D, Gradl D, Paulsen JE, Machonova O, Dembinski JL, Dinh H, Krauss S. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. doi: 10.1158/0008-5472.CAN-10-1282. PubMed PMID: 21199802.

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