Cat. No.: HY-117720A

OSU-2S TFA

Name: OSU-2S TFA
Brand: MedChemExpress
SKU: HY-117720A
Price: 1500.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

OSU-2S TFA is a non-immunosuppressive derivative of Fingolimod hydrochloride (FTY720) (HY-12005). It is an orally active, blood-brain barrier-permeable allosteric activator of PP2A that also activates PKCδ; it restores PP2A activity by displacing the inhibitory protein SET, thereby inducing ROS-PKCδ-caspase-3-dependent apoptosis, c-Myc degradation, cell cycle arrest, and differentiation. OSU-2S TFA is used in research on diseases such as leukemia, liver cancer, lymphoma, and lung cancer.

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화학식: C₂₃H₃₈F₃NO₄
분자량:449.55

보관:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

OSU-2S TFA Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]^[2]^[3]^[4]^[5]^[6]^[7]

PKCδ

All PKC Isoforms :

In Vitro

OSU-2S (2-6 μM; 24 h) TFA exhibits concentration-dependent cytotoxicity against canine B-cell lymphoma cell lines (CLBL-1 and 17–71)^[7].
The cytotoxicity of OSU-2S (3 μM; 24 h) TFA in canine B-cell lymphoma cell lines is partially mediated by ROS^[7].
OSU-2S (2-4 μM; 24 h) TFA induces ROS production and mediates cytotoxicity in primary cells from canine spontaneous B-cell lymphoma^[7].
OSU-2S (24 h) TFA downregulates PGC1α and inhibits mitochondrial biogenesis via PP2A-dependent FOXO1 dephosphorylation^[6].
OSU-2S TFA reduces mitochondrial mass and ATP production, and inhibits the expression of genes associated with mitochondrial biogenesis^[6].
OSU-2S (2 μM; 24 h) TFA induces apoptosis in primary CLL cells^[4].
OSU-2S TFA activates PP2A in CLL cells^[4].
OSU-2S (5 h) TFA induces SHP1 S591 phosphorylation via a PKC-dependent mechanism^[4].
OSU-2S (5-24 h) TFA -induced pSHP1 S591 levels correlate with CLL cell death^[4].
The cytotoxicity of OSU-2S (2 μM; 24 h) TFA is partially dependent on PKC^[4].
OSU-2S (8 μM; 4 h) TFA activates PKC in CLL cells^[4].
OSU-2S (8 μM; 16 h) TFA extensively regulates gene expression in CLL cells, affecting processes such as cell growth, proliferation, death, and the cell cycle^[4].
OSU-2S (8 μM; 16-24 h) TFA downregulates TCL1A expression in CLL cells^[4].
OSU-2S (5 μM; 24 h) TFA selectively kills CLL cells without affecting normal B cells via ROR1-targeted delivery^[4].
OSU-2S (2-8 μM; 24 h) TFA exhibits potent cytotoxicity against MCL cell lines^[3].
OSU-2S (2-8 μM; 24 h) TFA induces apoptosis in MCL cell lines^[3].
OSU-2S (4-5 μM; 24 h) TFA induces CD74 expression on the surface of MCL cells^[3].
OSU-2S (4 μM; 24 h) TFA enhances the cytotoxicity of Milatuzumab (HY-P99731) against MCL cells by upregulating CD74^[3].
OSU-2S (2-10 μM; 48 h) TFA demonstrates anti-proliferative activity against various HCC cell lines^[2].
OSU-2S (1.25-2.5 μM; 48 h) TFA enhances the anti-proliferative effect of Sorafenib (HY-10201) on HCC cells, exhibiting a synergistic effect^[2].
OSU-2S (1.25-2.5 μM; 48 h) TFA enhances Sorafenib-induced apoptosis in HCC cells^[2].
OSU-2S (1.25-2.5 μM; 48 h) TFA enhances the anti-HCC effect of Sorafenib via PKCδ and ERK pathways^[2].
OSU-2S (1.25-2.5 μM; 8-24 h) TFA in combination with Sorafenib inhibits HCC cell migration and invasion^[2].
The activity of OSU-2S (1.25-7.5 μM) TFA against HCC cells is influenced by p53 status; p53 restoration enhances sensitivity^[2].
OSU-2S (1-10 μM; 24 h) TFA inhibits A549 proliferation, with an IC₅₀ of 4.432 μM^[1].
OSU-2S (1.5-6 μM; 14 days) TFA inhibits colony formation in A549 cells^[1].
OSU-2S (1.5-6 μM; 12-24 h) TFA inhibits A549 cell migration^[1].
OSU-2S (1.5-6 μM; 24 h) TFA downregulates p-AURKA and S1PR1 protein expression in A549 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[7]

Cell Line:

Canine B-cell lymphoma cell lines CLBL-1 and 17-71
Concentration:

2 μM; 4 μM; 6 μM
Incubation Time:

24 h
Result:

Promoted cytotoxicity at concentrations as low as 2 μM.

Apoptosis Analysis^[7]

Cell Line:

Primary cells from canine spontaneous B-cell lymphoma
Concentration:

2 μM; 4 μM; 8 μM
Incubation Time:

24 h
Result:

Induced apoptosis in canine lymphoma cells.

Apoptosis Analysis^[4]

Cell Line:

Primary CD19+ cells from CLL patients
Concentration:

2 μM
Incubation Time:

24 h
Result:

Induced apoptosis in primary CLL cells.

RT-PCR^[4]

Cell Line:

CLL cells
Concentration:

8 μM
Incubation Time:

16 h
Result:

Reduced TCL1A mRNA levels.

Western Blot Analysis^[4]

Cell Line:

CLL cells
Concentration:

8 μM
Incubation Time:

24 h
Result:

Reduced TCL1A protein levels.

Apoptosis Analysis^[3]

Cell Line:

MCL cell line
Concentration:

5 μM
Incubation Time:

24 h
Result:

Induced apoptosis in MCL cell lines.

Cell Proliferation Assay^[2]

Cell Line:

Huh7, Hep3B, PLC5, HepG2
Concentration:

2 μM; 4 μM; 6 μM; 8 μM; 10 μM
Incubation Time:

48 h
Result:

Inhibited cell proliferation, with HepG2 being the most sensitive.

Cell Migration Assay ^[1]

Cell Line:

A549
Concentration:

1.5 μM; 3 μM; 6 μM
Incubation Time:

12 h; 24 h
Result:

Reduced the migration ability of A549 cells.

In Vivo

OSU-2S (2.5–10 mg/kg; intraperitoneal injection; every other day for 35 days) TFA inhibits tumor growth in an A549 xenograft model, is well tolerated, and downregulates Ki-67 and VEGF^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Subcutaneous inoculation of A549 cells into BALB/c nude mice^[1]
Dosage:

2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration:

i.p.; every other day for 35 days
Result:

Tumor volume and weight were significantly reduced.
There was no significant decrease in mouse body weight.
Immunohistochemistry showed that OSU-2S downregulated Ki-67 and VEGF.

Related Protocols :

Chemical Information

Appearance Solid
분자량 449.55
화학식 C₂₃H₃₈F₃NO₄
SMILES

CCC[C@@](CCC1=CC=C(OCCCCCC(C)C)C=C1)(N)CO.O=C(O)C(F)(F)F
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (1)

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Journal Impact Factor

Int Immunopharmacol

Osthole alleviates neuropathic pain by suppressing astrocytes activation and associated inflammatory responses via the PKCδ/TRPV4 signaling pathway. [Abstract]

2025 Sep 10:165:115453. PMID: 40934539

용액&용해도

In Vitro:

DMSO : 100 mg/mL (222.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2244 mL

11.1222 mL

22.2445 mL

5 mM

0.4449 mL

2.2244 mL

4.4489 mL

10 mM

0.2224 mL

1.1122 mL

2.2244 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Handling Instructions (2659 KB)

References

[1]. Han M, et al. Evaluation of the Efficacy of OSU-2S in the Treatment of Non-Small-Cell Lung Cancer and Screening of Potential Targets of Action. Pharmaceuticals (Basel). 2024 May 1;17(5):582.

[2]. Omar HA, et al. OSU-2S/Sorafenib Synergistic Antitumor Combination against Hepatocellular Carcinoma: The Role of PKCδ/p53. Front Pharmacol. 2016 Nov 30;7:463. [Content Brief]

[3]. Mani R, et al. ROR1-targeted delivery of OSU-2S, a nonimmunosuppressive FTY720 derivative, exerts potent cytotoxicity in mantle-cell lymphoma in vitro and in vivo. Exp Hematol. 2015 Sep;43(9):770-4.e2.

[4]. Mani R, et al. Tumor antigen ROR1 targeted drug delivery mediated selective leukemic but not normal B-cell cytotoxicity in chronic lymphocytic leukemia. Leukemia. 2015 Feb;29(2):346-55.

[5]. Xie Z, et al. Pharmacokinetics and Tolerability of the Novel Non-immunosuppressive Fingolimod Derivative, OSU-2S, in Dogs and Comparisons with Data in Mice and Rats. AAPS J. 2020 Jul 16;22(4):92.

[6]. Khalil SM, et al. Protein Phosphatase 2A Activation Dependent Down Regulation of PGC1-Alpha and FOXO1 Phosphorylation with OSU-2S in Human Lymphoma Cells. Blood. 2019;134(Supplement_1):3977.

[7]. Mani R, et al. Non-immunosuppressive FTY720-derivative OSU-2S mediates reactive oxygen species-mediated cytotoxicity in canine B-cell lymphoma. Vet Comp Oncol. 2017 Sep;15(3):1115-1118.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2244 mL	11.1222 mL	22.2445 mL	55.6112 mL
	5 mM	0.4449 mL	2.2244 mL	4.4489 mL	11.1222 mL
	10 mM	0.2224 mL	1.1122 mL	2.2244 mL	5.5611 mL
	15 mM	0.1483 mL	0.7415 mL	1.4830 mL	3.7074 mL
	20 mM	0.1112 mL	0.5561 mL	1.1122 mL	2.7806 mL
	25 mM	0.0890 mL	0.4449 mL	0.8898 mL	2.2244 mL
	30 mM	0.0741 mL	0.3707 mL	0.7415 mL	1.8537 mL
	40 mM	0.0556 mL	0.2781 mL	0.5561 mL	1.3903 mL
	50 mM	0.0445 mL	0.2224 mL	0.4449 mL	1.1122 mL
	60 mM	0.0371 mL	0.1854 mL	0.3707 mL	0.9269 mL
	80 mM	0.0278 mL	0.1390 mL	0.2781 mL	0.6951 mL
	100 mM	0.0222 mL	0.1112 mL	0.2224 mL	0.5561 mL

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OSU-2S TFA

1 Cited Publications

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OSU-2S TFA

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All PKC Isoforms