| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Integrin-linked kinase (ILK). OSU-T315 (1,5-regioisomer) is a novel, potent, and specific small molecule inhibitor of ILK with an IC50 of 0.6 μM. ILK is a serine/threonine protein kinase that plays a critical role in cell adhesion, migration, proliferation, and survival. It is a key component of the integrin signaling pathway and is involved in the regulation of the PI3K/AKT signaling pathway. By inhibiting ILK, OSU-T315 suppresses PI3K/AKT signaling through dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 also abrogates AKT activation by impeding AKT localization in lipid rafts. The compound triggers caspase-dependent apoptosis in an ILK-independent manner.
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| ln Vitro |
OSU-T315 (1,5-regioisomer) demonstrates potent inhibition of ILK with an IC50 of 0.6 μM. It suppresses cancer cell proliferation in vitro. The compound inhibits PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts. It triggers caspase-dependent apoptosis in an ILK-independent manner. The compound causes cell death through both apoptosis and autophagy. OSU-T315 has been shown to restrain tumor cell growth through regulating signaling pathways related to oncogenesis and tumor progression.
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| ln Vivo |
OSU-T315 (1,5-regioisomer) has been studied in vivo for its anti-tumor effects. It suppresses cancer cell proliferation in vivo. The compound inhibits PI3K/AKT signaling and causes cell death through apoptosis and autophagy. OSU-T315 has been found to restrain tumor cell growth in vivo through regulating signaling pathways related to oncogenesis and tumor progression. It is a potential therapeutic agent for leukemia. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical studies. OSU-T315 is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
ILK enzyme activity assays are performed using recombinant ILK enzyme and a peptide substrate. The enzyme is incubated with the substrate and [γ-³²P]ATP or fluorescently labeled ATP in kinase buffer (50 mM HEPES pH 7.5, 10 mM MgCl₂, 1 mM DTT) at 30°C for 30-60 minutes. Phosphorylated substrate is quantified by scintillation counting or fluorescence polarization. OSU-T315 is serially diluted in DMSO and added to the reaction mixture. The IC50 for ILK inhibition is 0.6 μM. Each concentration is tested in duplicate, and IC50 values are calculated by non-linear regression analysis. Appropriate positive controls (e.g., known ILK inhibitors) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cellular ILK inhibition is evaluated in cancer cell lines. Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with OSU-T315 at various concentrations for 24-72 hours. ILK activity in cell lysates is assessed by measuring phosphorylation of downstream targets (AKT-Ser473, GSK-3β) by Western blotting. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining, caspase-3/7 activity assays, and PARP cleavage Western blotting. Autophagy is assessed by LC3-II/I conversion and p62 degradation. Each experiment includes vehicle controls and appropriate positive controls to validate the assay systems.
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| Animal Protocol |
In vivo efficacy of OSU-T315 is evaluated in mouse xenograft models using human cancer cell lines, including leukemia models. Tumor cells are implanted subcutaneously in immunodeficient mice. When tumors reach a predetermined size, mice are randomized into treatment and control groups. OSU-T315 is administered orally or intraperitoneally at doses determined by preclinical studies. Tumor growth is monitored by caliper measurements. At study endpoint, tumors are harvested for histopathological analysis, immunohistochemistry (Ki67 for proliferation, cleaved caspase-3 for apoptosis), and biochemical assays (ILK activity, AKT phosphorylation). Body weight and clinical signs are monitored throughout the study to assess tolerability. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 533.6. Formula: C30H30F3N5O. CAS No.: 1333146-24-9. Synonyms: ILK inhibitor 22(1,5), T315(1,5). Appearance: White to light yellow solid powder. Density: 1.3±0.1 g/cm³. Boiling Point: 739.2±60.0 °C at 760 mmHg. LogP: 4.65. Solubility: Soluble in DMSO. Purity: ≥98%. OSU-T315 is a novel, potent, and specific ILK inhibitor with an IC50 of 0.6 μM.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for OSU-T315. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As an ILK inhibitor, potential toxicities may include effects on cell adhesion, migration, and proliferation. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References |
[3].OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics. J Immunol Res. 2018 Sep 12;2018:2505818. doi: 10.1155/2018/2505818. eCollection 2018. PubMed PMID: 30276218; PubMed Central PMCID: PMC6157143. |
| Additional Infomation |
OSU-T315 (1,5-regioisomer) is also known as ILK inhibitor 22(1,5), T315(1,5). Its IUPAC name is not fully resolved in publicly available sources. OSU-T315 is a novel, potent, and specific small molecule inhibitor of Integrin-linked kinase (ILK) with an IC50 of 0.6 μM. It suppresses cancer cell proliferation in vitro and in vivo and inhibits PI3K/AKT signaling. OSU-T315 triggers caspase-dependent apoptosis and causes cell death through apoptosis and autophagy. It is a potential therapeutic agent for leukemia. No clinical trials have been reported for this compound. OSU-T315 is for research use only.
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| Molecular Formula |
C30H30F3N5O
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|---|---|
| Molecular Weight |
533.6
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| Exact Mass |
533.24
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| CAS # |
1333146-24-9
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| Related CAS # |
1333146-24-9;
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| PubChem CID |
51051074
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
739.2±60.0 °C at 760 mmHg
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| Flash Point |
400.9±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
4.65
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
767
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC(=O)CCC1=NN(C(=C1)C2=CC=C(C=C2)C3=CC=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)N5CCNCC5
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| InChi Key |
GHBUPSVATJKTRR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H30F3N5O/c1-34-29(39)15-10-25-20-28(38(36-25)27-13-11-26(12-14-27)37-18-16-35-17-19-37)23-4-2-21(3-5-23)22-6-8-24(9-7-22)30(31,32)33/h2-9,11-14,20,35H,10,15-19H2,1H3,(H,34,39)
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| Chemical Name |
N-Methyl-3-[1-(4-piperazin-1-yl-phenyl)-5-(4'-trifluoromethyl-biphenyl-4-yl)-1H-pyrazol-3-yl]-propionamide
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| Synonyms |
ILK inhibitor 22(1,5) T315(1,5) OSU-T315 (1,5-regioisomer) OSUT315 OSU T315 OSU-T315
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~93.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (9.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8741 mL | 9.3703 mL | 18.7406 mL | |
| 5 mM | 0.3748 mL | 1.8741 mL | 3.7481 mL | |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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