WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H565003
CAS#: 6975-75-3
Description: QLT0267 is an ATP-competitive selective inhibitor of integrin-linked kinase (ILK).
Hodoodo Cat#: H565003
Name: QLT0267
CAS#: 6975-75-3
Chemical Formula: C10H12N6O
Exact Mass: 232.11
Molecular Weight: 232.250
Elemental Analysis: C, 51.72; H, 5.21; N, 36.19; O, 6.89
Related CAS #: 6975-75-3 866409-68-9
Synonym: QLT-0267; QLT 0267; QLT0267; QLT-267; QLT 267; QLT267; NSC 21678; NSC-21678; NSC21678; ILK-IN-3;
IUPAC/Chemical Name: 4-(4-Methoxy-phenylazo)-1H-pyrazole-3,5-diamine
InChi Key: QNRNTYHAOBVOKW-BUHFOSPRSA-N
InChi Code: InChI=1S/C10H12N6O/c1-17-7-4-2-6(3-5-7)13-14-8-9(11)15-16-10(8)12/h2-5H,1H3,(H5,11,12,15,16)/b14-13+
SMILES Code: NC1=NNC(N)=C1/N=N/C2=CC=C(OC)C=C2
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
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:
| Biological target: | QLT0267 is an ATP-competitive selective inhibitor of integrin-linked kinase (ILK). |
| In vitro activity: | ILK inhibitor QLT0267 also reduced desmin protein expression and elevated nephrin protein expression in high glucose (HG) stimulated podocytes (Fig. 1). Immunofluorescence analysis further confirmed that HG induced an increment in desmin expression in podocytes. However, the HG-induced increase in desmin expression was alleviated by QLT0267 treatment (Fig. 2). Reference: Cell Physiol Biochem. 2015;35(4):1425-36. https://www.karger.com/?DOI=10.1159/000373963 |
| In vivo activity: | As shown in Figure 4, blood glucose (BG) level was significantly higher in diabetic rats compared with nondiabetic control animals. However, no differences in BG level was observed between EMO treated and untreated STZ-induced diabetic rats (Fig. 4A). Moreover, the STZ-induced diabetic rats showed severe urinary albumin/creatinine ratio (ACR) when compared with the nornmal control rats (P < 0.05). However, treatment with QLT0267 significantly reduced urinary ACR (expressed as mg/g Cr ) in STZ-induced diabetic rats (Fig. 4B). Reference: Cell Physiol Biochem. 2015;35(4):1425-36. https://www.karger.com/?DOI=10.1159/000373963 |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.0 | 129.17 |
The following data is based on the product molecular weight 232.25 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: | |
| In vitro protocol: | 1. Chen T, Zheng LY, Xiao W, Gui D, Wang X, Wang N. Emodin ameliorates high glucose induced-podocyte epithelial-mesenchymal transition in-vitro and in-vivo. Cell Physiol Biochem. 2015;35(4):1425-36. doi: 10.1159/000373963. Epub 2015 Mar 12. PMID: 25791065. 2. Eke I, Leonhardt F, Storch K, Hehlgans S, Cordes N. The small molecule inhibitor QLT0267 Radiosensitizes squamous cell carcinoma cells of the head and neck. PLoS One. 2009 Jul 30;4(7):e6434. doi: 10.1371/journal.pone.0006434. PMID: 19649326; PMCID: PMC2713401. |
| In vivo protocol: | 1. Chen T, Zheng LY, Xiao W, Gui D, Wang X, Wang N. Emodin ameliorates high glucose induced-podocyte epithelial-mesenchymal transition in-vitro and in-vivo. Cell Physiol Biochem. 2015;35(4):1425-36. doi: 10.1159/000373963. Epub 2015 Mar 12. PMID: 25791065. |
1: Chadla P, Arbi M, Nikou S, Kalliakoudas T, Papadaki H, Taraviras S, Lygerou Z, Bravou V. Integrin-Linked-Kinase Overexpression Is Implicated in Mechanisms of Genomic Instability in Human Colorectal Cancer. Dig Dis Sci. 2020 Jun 3. doi: 10.1007/s10620-020-06364-6. Epub ahead of print. PMID: 32495257.
2: Tan J, Digicaylioglu M, Wang SXJ, Dresselhuis J, Dedhar S, Mills J. Insulin attenuates apoptosis in neuronal cells by an integrin-linked kinase-dependent mechanism. Heliyon. 2019 Aug 16;5(8):e02294. doi: 10.1016/j.heliyon.2019.e02294. PMID: 31463398; PMCID: PMC6706370.
3: Fang CC, Chou TH, Huang JW, Lee CC, Chen SC. The Small Molecule Inhibitor QLT-0267 Decreases the Production of Fibrin-Induced Inflammatory Cytokines and Prevents Post-Surgical Peritoneal Adhesions. Sci Rep. 2018 Jun 21;8(1):9481. doi: 10.1038/s41598-018-25994-5. PMID: 29930281; PMCID: PMC6013455.
4: Li Y, Li G, Hu X, Lin W, Sun J, Mi L, Wang R, Wang J, Wang X, Zhou R. Integrin-Linked Kinase Senses Hypoxia During Scar Angiogenesis. Int J Low Extrem Wounds. 2016 Dec;15(4):286-295. doi: 10.1177/1534734616649485. Epub 2016 Jun 23. PMID: 27230895.
5: Li G, Li YY, Sun JE, Lin WH, Zhou RX. ILK-PI3K/AKT pathway participates in cutaneous wound contraction by regulating fibroblast migration and differentiation to myofibroblast. Lab Invest. 2016 Jul;96(7):741-51. doi: 10.1038/labinvest.2016.48. Epub 2016 Apr 25. PMID: 27111285.
6: Du M, Wang Q, Li W, Ma X, Wu L, Guo F, Zhao S, Huang F, Wang H, Qin G. Overexpression of FOXO1 ameliorates the podocyte epithelial-mesenchymal transition induced by high glucose in vitro and in vivo. Biochem Biophys Res Commun. 2016 Mar 18;471(4):416-22. doi: 10.1016/j.bbrc.2016.02.066. Epub 2016 Feb 19. PMID: 26902117.
7: Duminuco R, Noble JW, Goody J, Sharma M, Ksander BR, Roskelley CD, Cox ME, Mills J. Integrin-linked kinase regulates senescence in an Rb-dependent manner in cancer cell lines. Cell Cycle. 2015;14(18):2924-37. doi: 10.1080/15384101.2015.1064205. PMID: 26176204; PMCID: PMC4825635.
8: Kalra J, Dragowska WH, Bally MB. Using Pharmacokinetic Profiles and Digital Quantification of Stained Tissue Microarrays as a Medium-Throughput, Quantitative Method for Measuring the Kinetics of Early Signaling Changes Following Integrin-Linked Kinase Inhibition in an In Vivo Model of Cancer. J Histochem Cytochem. 2015 Sep;63(9):691-709. doi: 10.1369/0022155415587978. Epub 2015 May 4. PMID: 25940338; PMCID: PMC4804727.
9: Chen T, Zheng LY, Xiao W, Gui D, Wang X, Wang N. Emodin ameliorates high glucose induced-podocyte epithelial-mesenchymal transition in-vitro and in-vivo. Cell Physiol Biochem. 2015;35(4):1425-36. doi: 10.1159/000373963. Epub 2015 Mar 12. PMID: 25791065.
10: Bhakta-Guha D, Saeed ME, Greten HJ, Efferth T. Dis-organizing centrosomal clusters: specific cancer therapy for a generic spread? Curr Med Chem. 2015;22(6):685-94. doi: 10.2174/0929867322666141212114529. PMID: 25515519.
11: Sikkema WK, Strikwerda A, Sharma M, Assi K, Salh B, Cox ME, Mills J. Regulation of mitotic cytoskeleton dynamics and cytokinesis by integrin-linked kinase in retinoblastoma cells. PLoS One. 2014 Jun 9;9(6):e98838. doi: 10.1371/journal.pone.0098838. PMID: 24911651; PMCID: PMC4049663.
12: Jones CI, Tucker KL, Sasikumar P, Sage T, Kaiser WJ, Moore C, Emerson M, Gibbins JM. Integrin-linked kinase regulates the rate of platelet activation and is essential for the formation of stable thrombi. J Thromb Haemost. 2014 Aug;12(8):1342-52. doi: 10.1111/jth.12620. Epub 2014 Jul 31. PMID: 24888521.
13: Ernst N, Yay A, Bíró T, Tiede S, Humphries M, Paus R, Kloepper JE. β1 integrin signaling maintains human epithelial progenitor cell survival in situ and controls proliferation, apoptosis and migration of their progeny. PLoS One. 2013 Dec 27;8(12):e84356. doi: 10.1371/journal.pone.0084356. PMID: 24386370; PMCID: PMC3874009.
14: Li Y, Zhang J, Yan H. Integrin-linked kinase inhibition attenuates permeability of the streptozotocin-induced diabetic rat retina. Cell Biochem Biophys. 2013;67(3):1467-72. doi: 10.1007/s12013-013-9647-z. PMID: 23712867.
15: Yu L, Yuan X, Wang D, Barakat B, Williams ED, Hannigan GE. Selective regulation of p38β protein and signaling by integrin-linked kinase mediates bladder cancer cell migration. Oncogene. 2014 Feb 6;33(6):690-701. doi: 10.1038/onc.2013.20. Epub 2013 Feb 25. PMID: 23435415.
16: Lim S, Kawamura E, Fielding AB, Maydan M, Dedhar S. Integrin-linked kinase regulates interphase and mitotic microtubule dynamics. PLoS One. 2013;8(1):e53702. doi: 10.1371/journal.pone.0053702. Epub 2013 Jan 21. PMID: 23349730; PMCID: PMC3549953.
17: Becker-Santos DD, Guo Y, Ghaffari M, Vickers ED, Lehman M, Altamirano-Dimas M, Oloumi A, Furukawa J, Sharma M, Wang Y, Dedhar S, Cox ME. Integrin-linked kinase as a target for ERG-mediated invasive properties in prostate cancer models. Carcinogenesis. 2012 Dec;33(12):2558-67. doi: 10.1093/carcin/bgs285. Epub 2012 Oct 1. PMID: 23027626; PMCID: PMC3510737.
18: Steinbrunn T, Siegmund D, Andrulis M, Grella E, Kortüm M, Einsele H, Wajant H, Bargou RC, Stühmer T. Integrin-linked kinase is dispensable for multiple myeloma cell survival. Leuk Res. 2012 Sep;36(9):1165-71. doi: 10.1016/j.leukres.2012.05.005. Epub 2012 Jun 1. PMID: 22658851.
19: Kalra J, Anantha M, Warburton C, Waterhouse D, Yan H, Yang YJ, Strut D, Osooly M, Masin D, Bally MB. Validating the use of a luciferase labeled breast cancer cell line, MDA435LCC6, as a means to monitor tumor progression and to assess the therapeutic activity of an established anticancer drug, docetaxel (Dt) alone or in combination with the ILK inhibitor, QLT0267. Cancer Biol Ther. 2011 May 1;11(9):826-38. doi: 10.4161/cbt.11.9.15183. Epub 2011 May 1. PMID: 21358264; PMCID: PMC3100631.
20: Faralli JA, Newman JR, Sheibani N, Dedhar S, Peters DM. Integrin-linked kinase regulates integrin signaling in human trabecular meshwork cells. Invest Ophthalmol Vis Sci. 2011 Mar 25;52(3):1684-92. doi: 10.1167/iovs.10-6397. PMID: 21071740; PMCID: PMC3101682.
