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MedKoo Cat#: 406831 | Name: WZ4003
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Description:

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

WZ4003 is a selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. WZ4003 inhibits both NUAK isoforms (IC50 for NUAK1 is 20 nM and for NUAK2 is 100 nM). WZ4003 displays extreme selectivity and do not significantly inhibit the activity of 139 other kinases that were tested including ten AMPK family members. In all cell lines tested, WZ4003 inhibits the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser(445).

Chemical Structure

WZ4003
WZ4003
CAS#1214265-58-3

Theoretical Analysis

MedKoo Cat#: 406831

Name: WZ4003

CAS#: 1214265-58-3

Chemical Formula: C25H29ClN6O3

Exact Mass: 496.1990

Molecular Weight: 497.00

Elemental Analysis: C, 60.42; H, 5.88; Cl, 7.13; N, 16.91; O, 9.66

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 150.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,650.00 Ready to ship
1g USD 2,950.00 Ready to ship
2g USD 5,250.00 Ready to ship
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Related CAS #
No Data
Synonym
WZ4003; WZ-4003; WZ 4003.
IUPAC/Chemical Name
N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide
InChi Key
SDGJBAUIGHSMRI-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H29ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h5-9,14-16H,4,10-13H2,1-3H3,(H,28,33)(H,27,29,30)
SMILES Code
CCC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O
Appearance
White to beige 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
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
Biological target:
WZ4003 is a NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2.
In vitro activity:
The structure of WZ4003 is shown in Figure 1(A). It inhibits NUAK1 with an IC50 of 20 nM (Figure 1B) and NUAK2 with an IC50 of 100 nM (Figure 1B). To evaluate the specificity of WZ4003 this study studied the effect that this compound has on the activity of 140 protein kinases, including ten AMPK-related kinase family members most closely related to NUAK1 (Figure 1C and Supplementary Table S1). WZ4003 was remarkably specific and, apart from NUAK1 and NUAK2, did not significantly inhibit ten other AMPK-related kinases or other kinases tested, including LKB1 at a concentration of 1 μM (10-fold higher than the IC50 of inhibition of NUAK1). Reference: Biochem J. 2014 Jan 1; 457(Pt 1): 215–225. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3969223/
In vivo activity:
N/A
Solvent mg/mL mM
Solubility
DMSO 16.1 32.33
DMF 14.0 28.17
DMF:PBS (pH 7.2) (1:1) 0.5 1.01
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 497.00 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.

Recalculate based on batch purity %
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. Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.
In vitro protocol:
1. Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.
In vivo protocol:
N/A
1: Taylor LW, Simzer EM, Pimblett C, Lacey-Solymar OTT, McGeachan RI, Meftah S, Rose JL, Spires-Jones MP, Holt K, Catterson JH, Koch H, Liaquat I, Clarke JH, Skidmore J, Smith C, Booker SA, Brennan PM, Spires-Jones TL, Durrant CS. p-tau Ser356 is associated with Alzheimer's disease pathology and is lowered in brain slice cultures using the NUAK inhibitor WZ4003. Acta Neuropathol. 2024 Jan 4;147(1):7. doi: 10.1007/s00401-023-02667-w. PMID: 38175261; PMCID: PMC10766794. 2: Xiang T, Wei Z, Ye C, Liu G. Prognostic impact and immunotherapeutic implications of NETosis-related gene signature in gastric cancer patients. J Cell Mol Med. 2024 Mar;28(5):e18087. doi: 10.1111/jcmm.18087. Epub 2023 Dec 26. PMID: 38146607; PMCID: PMC10902305. 3: Liu Y, Wang R, Huang R, Rutz B, Ciotkowska A, Tamalunas A, Hu S, Trieb M, Waidelich R, Strittmatter F, Stief CG, Hennenberg M. Inhibition of growth and contraction in human prostate stromal cells by silencing of NUAK1 and -2, and by the presumed NUAK inhibitors HTH01-015 and WZ4003. Front Pharmacol. 2023 Apr 28;14:1105427. doi: 10.3389/fphar.2023.1105427. PMID: 37188272; PMCID: PMC10175612. 4: Tsai HW, Li CJ, Lin LT, Chiang AJ, Chen SN, Wen ZH, Tsui KH. Expression status and prognostic significance of mitochondrial dynamics OPA3 in human ovarian cancer. Aging (Albany NY). 2022 May 4;14(9):3874-3886. doi: 10.18632/aging.204050. Epub 2022 May 4. PMID: 35507809; PMCID: PMC9134952. 5: Almalki FA, Shawky AM, Abdalla AN, Gouda AM. Icotinib, Almonertinib, and Olmutinib: A 2D Similarity/Docking-Based Study to Predict the Potential Binding Modes and Interactions into EGFR. Molecules. 2021 Oct 24;26(21):6423. doi: 10.3390/molecules26216423. PMID: 34770832; PMCID: PMC8588130. 6: Chen J, Zhang S, Zheng X, Mao J, Xie S, Chen W, Ran X. WZ4003 sensitizes non- small cell lung cancer cells to gefitinib via inhibition of ARK5 and epithelial- to-mesenchymal transition. Am J Transl Res. 2020 Nov 15;12(11):7377-7385. PMID: 33312374; PMCID: PMC7724321. 7: Yang H, Wang X, Wang C, Yin F, Qu L, Shi C, Zhao J, Li S, Ji L, Peng W, Luo H, Cheng M, Kong L. Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer. Eur J Med Chem. 2021 Jan 15;210:113080. doi: 10.1016/j.ejmech.2020.113080. Epub 2020 Dec 4. PMID: 33310286. 8: Pu Y, Wang M, Hong Y, Wu Y, Tang Z. Adiponectin promotes human jaw bone marrow mesenchymal stem cell chemotaxis via CXCL1 and CXCL8. J Cell Mol Med. 2017 Jul;21(7):1411-1419. doi: 10.1111/jcmm.13070. Epub 2017 Feb 8. PMID: 28176455; PMCID: PMC5487911. 9: Banerjee S, Zagórska A, Deak M, Campbell DG, Prescott AR, Alessi DR. Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase. Biochem J. 2014 Jul 15;461(2):233-45. doi: 10.1042/BJ20140408. PMID: 24785407; PMCID: PMC4109838. 10: Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.