ILK-IN-2 (Synonyms: OSU-T315 analog)

Name: ILK-IN-2
Brand: MedChemExpress
SKU: HY-18676B
Rating: 4.5 (1 reviews)

Cat. No.: HY-18676B Purity: 98.79%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

ILK-IN-2 Chemical Structure

CAS No. : 1333146-24-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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100 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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View All Isoforms

Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ILK

0.6 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	1.6 μM Compound: 22	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	[PMID: 21823616]
MCF7	IC₅₀	2.5 μM Compound: 22	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	[PMID: 21823616]
MDA-MB-231	IC₅₀	1 μM Compound: 22	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	[PMID: 21823616]
MDA-MB-468	IC₅₀	1.5 μM Compound: 22	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	[PMID: 21823616]
PC-3	IC₅₀	2 μM Compound: 22	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	[PMID: 21823616]
SK-BR-3	IC₅₀	1.8 μM Compound: 22	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	[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.

Cell Viability Assay^[1]

Cell Line:	Mec-1, OSU-CLL, B cell, T cell
Concentration:	0, 2, 4, 6, 8, 10 μM; 0, 1, 2, 3, 4, 5 μM
Incubation Time:	24 h
Result:	Had dose-dependent cytotoxicity against CLL cells, while its cytotoxicity was reduced in normal T cells and B cells.

Apoptosis Analysis^[1]

Cell Line:	CLL
Concentration:	4 μM
Incubation Time:	16 h
Result:	Reversed the elevated levels of Mcl-1, significantly enhancing caspase 3/7 activity.

Western Blot Analysis^[1]

Cell Line:	Mec-1, OSU-CLL
Concentration:	1, 2, 3, 4 μM
Incubation Time:	15 min
Result:	Did not disrupt PDK1 phosphorylation, PI3 kinase activity or the activity of Ras interactions with proto-oncogene serine/threonine protein kinases.

Western Blot Analysis^[2]

Cell Line:	PC3, MDA-MB-231
Concentration:	0, 1, 2, 3, 4 μM; 0, 0.5, 1, 1.5, 2, 2.5 μM
Incubation Time:	24 h
Result:	Showed dose-dependent inhibition of Akt phosphorylation.

Apoptosis Analysis^[2]

Cell Line:	PC-3
Concentration:	0, 1, 2, 3, 4 μM
Incubation Time:	24 h
Result:	Induced cell apoptosis and autophagy simultaneously, and autophagy occured before cell apoptosis.

In Vivo

ILK-IN-2 (25-50 mg/kg, oral or intraperitoneal injection, once daily, 2-4 weeks) delays leukemia progression in mice and significantly improves the overall survival rate of mice harboring TCL1 leukemia cells^{[ 1 ]}.
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.

Animal Model:	Pharmacokinetic properties of OSU-T315^[1]
Dosage:	50 mg/kg, daily for 4 weeks; 25 mg/kg, once daily for 2 weeks
Administration:	Oral; Intraperitoneal injection (i.p.)
Result:	Reduced white blood cell count and prolonged the survival of mice.

Animal Model:	PC-3 tumor xenograft mice model^[2]
Dosage:	25, 50 mg/kg; daily; 35 days
Administration:	Oral
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.

Molecular Weight

533.59

Formula

C₃₀H₃₀F₃N₅O

CAS No.

1333146-24-9

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8741 mL	9.3705 mL	18.7410 mL
5 mM	0.3748 mL	1.8741 mL	3.7482 mL
10 mM	0.1874 mL	0.9370 mL	1.8741 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (9.37 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.41%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (251 KB) LCMS (123 KB)

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

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

ILK-IN-2 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ILK-IN-21333146-24-9OSU-T315IntegrinAutophagyApoptosisCaspasePDHKPyruvate dehydrogenase kinasePDH kinaseAnti-tumorapoptosisautophagyoralchronic lymphocytic leukemiaInhibitorinhibitorinhibit

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ILK-IN-2 (Synonyms: OSU-T315 analog)

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ILK-IN-2 Related Antibodies

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Biological Activity

Purity & Documentation

References

Customer Review

ILK-IN-2 Related Antibodies

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Complete Stock Solution Preparation Table

ILK-IN-2 Related Classifications

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