ILK-IN-2
Based on 1 Customer Validation
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models.
For research use only. We do not sell to patients.
- Purity : 98.79%
- CAS No.: 1333146-24-9
- Formula: C30H30F3N5O
- Molecular Weight:533.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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ILK 0.6 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| LNCaP | IC50 |
1.6 μM
Compound: 22
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Antiproliferative activity against human LNCAP cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human LNCAP cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
| MCF7 | IC50 |
2.5 μM
Compound: 22
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Antiproliferative activity against human MCF7 cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human MCF7 cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
| MDA-MB-231 | IC50 |
1 μM
Compound: 22
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Antiproliferative activity against human MDA-MB-231 cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
| MDA-MB-468 | IC50 |
1.5 μM
Compound: 22
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Antiproliferative activity against human MDA-MB-468 cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
| PC-3 | IC50 |
2 μM
Compound: 22
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Antiproliferative activity against human PC3 cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human PC3 cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
| SK-BR-3 | IC50 |
1.8 μM
Compound: 22
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Antiproliferative activity against human SKBR3 cells assessed as suppression of cell viability by MTT assay
Antiproliferative activity against human SKBR3 cells assessed as suppression of cell viability by MTT assay
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[PMID: 21823616] |
In Vitro
ILK-IN-2 (0-10 μM, 24 h) shows dose-dependent selective cytotoxicity on CLL-derived cell lines and primary CLL cells, but has minimal impact on normal lymphocytes[1].
ILK-IN-2 (4 μM, 16 h) reduces levels of Mcl-1 and Bcl-xl in CLL cells, triggering caspase activation within those cells[1].
ILK-IN-2 (1-4 μM, 15 min) does not affect proximal membrane signaling of AKT in Mec-1 and OSU-CLL cells[1].
ILK-IN-2 (0-5 μM, 24 h) inhibits the proliferation of prostate and breast cancer cell lines, with IC50 values for LNCaP, PC-3, MDA-MB-231, MDA-MB-468, SKBR3, and MCF-7 being 1.6, 2, 1, 1.5, 1.8, and 2.5 μM respectively, while having no effect on normal epithelial cells[2].
ILK-IN-2 (0-4 μM, 24 h) inhibits PDK2 in PC3 and MDA-MB-231 by suppressing the phosphorylation of Akt at the Ser-473 site[2].
ILK-IN-2 (0-4 μM, 24 h) induces cell death in PC-3 cells through autophagy and apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Mec-1, OSU-CLL, B cell, T cell
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Concentration:0, 2, 4, 6, 8, 10 μM; 0, 1, 2, 3, 4, 5 μM
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Incubation Time:24 h
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Result:Had dose-dependent cytotoxicity against CLL cells, while its cytotoxicity was reduced in normal T cells and B cells.
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Cell Line:CLL
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Concentration:4 μM
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Incubation Time:16 h
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Result:Reversed the elevated levels of Mcl-1, significantly enhancing caspase 3/7 activity.
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Cell Line:Mec-1, OSU-CLL
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Concentration:1, 2, 3, 4 μM
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Incubation Time:15 min
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Result:Did not disrupt PDK1 phosphorylation, PI3 kinase activity or the activity of Ras interactions with proto-oncogene serine/threonine protein kinases.
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Cell Line:PC3, MDA-MB-231
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Concentration:0, 1, 2, 3, 4 μM; 0, 0.5, 1, 1.5, 2, 2.5 μM
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Incubation Time:24 h
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Result:Showed dose-dependent inhibition of Akt phosphorylation.
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Cell Line:PC-3
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Concentration:0, 1, 2, 3, 4 μM
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Incubation Time:24 h
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Result:Induced cell apoptosis and autophagy simultaneously, and autophagy occured before cell apoptosis.
In Vivo
ILK-IN-2 (25-50 mg/kg, orally, daily, for 35 days) inhibits the growth of PC-3 xenograft tumors in nude mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pharmacokinetic properties of OSU-T315[1]
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Dosage:50 mg/kg, daily for 4 weeks; 25 mg/kg, once daily for 2 weeks
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Administration:Oral; Intraperitoneal injection (i.p.)
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Result:Reduced white blood cell count and prolonged the survival of mice.
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Animal Model:PC-3 tumor xenograft mice model[2]
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Dosage:25, 50 mg/kg; daily; 35 days
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Administration:Oral
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Result:Significantly inhibited tumor growth (25 and 50 mg/kg groups inhibited 48% and 62% respectively).
Showed that the phosphorylation of Ser-473-Akt was dose-dependently inhibited, while the phosphorylation of Thr-308-Akt was not affected. At the same time, the phosphorylation levels of GSK3β and MLC and the expression levels of YB-1, HER2 and EGFR also appeared in parallel decline.
Chemical Information
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CAS No. 1333146-24-9
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Appearance Solid
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Molecular Weight 533.59
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Formula C30H30F3N5O
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Color White to light yellow
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SMILES
O=C(NC)CCC1=NN(C2=CC=C(N3CCNCC3)C=C2)C(C4=CC=C(C5=CC=C(C(F)(F)F)C=C5)C=C4)=C1
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Synonyms
OSU-T315 analog
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (93.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.37 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Ta-Ming Liu, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. [Content Brief]
[2]. Su-Lin Lee, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8741 mL | 9.3705 mL | 18.7410 mL | 46.8524 mL |
| 5 mM | 0.3748 mL | 1.8741 mL | 3.7482 mL | 9.3705 mL | |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL | 4.6852 mL | |
| 15 mM | 0.1249 mL | 0.6247 mL | 1.2494 mL | 3.1235 mL | |
| 20 mM | 0.0937 mL | 0.4685 mL | 0.9370 mL | 2.3426 mL | |
| 25 mM | 0.0750 mL | 0.3748 mL | 0.7496 mL | 1.8741 mL | |
| 30 mM | 0.0625 mL | 0.3123 mL | 0.6247 mL | 1.5617 mL | |
| 40 mM | 0.0469 mL | 0.2343 mL | 0.4685 mL | 1.1713 mL | |
| 50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL | 0.9370 mL | |
| 60 mM | 0.0312 mL | 0.1562 mL | 0.3123 mL | 0.7809 mL | |
| 80 mM | 0.0234 mL | 0.1171 mL | 0.2343 mL | 0.5857 mL |
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