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OSU-2S

Name: OSU-2S
Brand: MedChemExpress
SKU: HY-117720
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OSU-2S 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 is used in research on diseases such as leukemia, liver cancer, lymphoma, and lung cancer.

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No. CAS: 1351056-65-9
Fòrmula: C₂₁H₃₇NO₂
Peso molecular:335.52

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (294 KB)

OSU-2S Chemical Structure

No. CAS: 1351056-65-9

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

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

PKCδ

Ver todos los productos específicos de isoformas PKC :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4.2 μM Compound: OSU-2S	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 28865276]
Hep 3B2	IC₅₀	2.8 μM Compound: OSU-2S	Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay	[PMID: 28865276]
HepG2	IC₅₀	2.3 μM Compound: OSU-2S	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 28865276]
HT-29	IC₅₀	2.7 μM Compound: OSU-2S	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 28865276]

In Vitro

Anti-cancerOxidative StressMitochondrial FunctionApoptosisCell Cycle RegulationOthers

Anti-cancer

OSU-2S (2-6 μM; 24 h) exhibits concentration-dependent cytotoxicity against canine B-cell lymphoma cell lines (CLBL-1 and 17-71)^[7].
OSU-2S activates PP2A in CLL cells^[4].
OSU-2S (5-24 h)-induced pSHP1 S591 levels correlate with CLL cell death^[4].
OSU-2S (8 μM; 4 h) activates PKC in CLL cells^[4].
OSU-2S (8 μM; 16-24 h) downregulates TCL1A expression in CLL^[4].
OSU-2S (5 μM; 24 h) selectively kills CLL cells without killing normal B cells via ROR1-targeted delivery^[4].
OSU-2S (2-8 μM; 24 h) exhibits strong cytotoxicity against MCL cell lines^[3].
OSU-2S (4-5 μM; 24 h) induces CD74 surface expression in MCL cells^[3].
OSU-2S (4 μM; 24 h) enhances the cytotoxicity of Milatuzumab (HY-P99731) against MCL by upregulating CD74^[3].
OSU-2S (2-10 μM; 48 h) exhibits antiproliferative activity against multiple HCC cell lines^[2].
OSU-2S (1.25-2.5 μM; 48 h) enhances the antiproliferative effect of Sorafenib (HY-10201) on HCC cells and exhibits a synergistic effect^[2].
OSU-2S (1.25-2.5 μM; 48 h) enhances the anti-HCC effect of Sorafenib through the PKCδ and ERK pathways^[2].
OSU-2S (1.25-2.5 μM; 8-24 h) in combination with Sorafenib inhibits HCC cell migration and invasion^[2].
OSU-2S (1.25-7.5 μM) activity against HCC cells is influenced by p53 status, and p53 restoration enhances sensitivity^[2].
OSU-2S (1-10 μM; 24 h) inhibits A549 proliferation with an IC₅₀ of 4.432 μM^[1].
OSU-2S (1.5-6 μM; 14 days) inhibits colony formation in A549 cells^[1].
OSU-2S (1.5-6 μM; 12-24 h) inhibits A549 cell migration^[1].
OSU-2S (1.5-6 μM; 24 h) downregulates p-AURKA and S1PR1 protein expression in A549 cells^[1].

Anti-cancer

Oxidative Stress

OSU-2S (3 μM; 24 h) cytotoxicity in canine B-cell lymphoma cell lines is partially mediated by ROS^[7].
OSU-2S (2-4 μM; 24 h) induces ROS production and mediates cytotoxicity in primary canine spontaneous B-cell lymphoma cells^[7].

Mitochondrial Function

OSU-2S (24 h) downregulates PGC1α through PP2A-dependent FOXO1 dephosphorylation and inhibits mitochondrial biogenesis^[6].
OSU-2S reduces mitochondrial mass and ATP production, and inhibits the expression of genes related to mitochondrial biogenesis^[6].

Anti-cancer

Apoptosis

OSU-2S (2 μM; 24 h) induces apoptosis in primary CLL cells^[4].
OSU-2S (2-8 μM; 24 h) induces apoptosis in MCL cell lines^[3].
OSU-2S (1.25-2.5 μM; 48 h) enhances Sorafenib-induced apoptosis in HCC cells^[2].

Anti-cancer

Cell Cycle Regulation

OSU-2S (8 μM; 16 h) broadly regulates gene expression in CLL cells, involving cell growth, proliferation, death, and cycle^[4].

Others

OSU-2S (5 h) induces SHP1 S591 phosphorylation through a PKC-dependent mechanism^[4].
OSU-2S (2 μM; 24 h) cytotoxicity is partially dependent on PKC^[4].

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

Anti-cancer

OSU-2S (2.5-10 mg/kg; intraperitoneal injection; once every other day for 35 days) inhibited tumor growth in the A549 xenograft model, was well tolerated, and downregulated 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

No. CAS 1351056-65-9
Peso molecular 335.52
Fòrmula C₂₁H₃₇NO₂
SMILES

CCC[C@@](CCC1=CC=C(OCCCCCC(C)C)C=C1)(N)CO
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (294 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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.

Calculators

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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.

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OSU-2S

1 Cited Publications

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OSU-2S

Publications Citing Use of MedChemExpress (MCE) OSU-2S

Ver todos los productos específicos de isoformas PKC