Cat. No.: HY-117720

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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.

For research use only. We do not sell to patients.

CAS No.: 1351056-65-9
Formula: C₂₁H₃₇NO₂
Molecular Weight:335.52

Storage:

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

Data Sheet (294 KB)

OSU-2S Chemical Structure

CAS No.: 1351056-65-9

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

PKCδ

All PKC Isoforms :

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

OSU-2S (2-6 μM; 24 h) 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) 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 cells from canine spontaneous B-cell lymphoma^[7].
OSU-2S (24 h) downregulates PGC1α and inhibits mitochondrial biogenesis via PP2A-dependent FOXO1 dephosphorylation^[6].
OSU-2S reduces mitochondrial mass and ATP production, and inhibits the expression of genes associated with mitochondrial biogenesis^[6].
OSU-2S (2 μM; 24 h) induces apoptosis in primary CLL cells^[4].
OSU-2S activates PP2A in CLL cells^[4].
OSU-2S (5 h) induces SHP1 S591 phosphorylation via a PKC-dependent mechanism^[4].
OSU-2S (5-24 h)-induced pSHP1 S591 levels correlate with CLL cell death^[4].
The cytotoxicity of OSU-2S (2 μM; 24 h) is partially dependent on PKC^[4].
OSU-2S (8 μM; 4 h) activates PKC in CLL cells^[4].
OSU-2S (8 μM; 16 h) 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) downregulates TCL1A expression in CLL cells^[4].
OSU-2S (5 μM; 24 h) selectively kills CLL cells without affecting normal B cells via ROR1-targeted delivery^[4].
OSU-2S (2-8 μM; 24 h) exhibits potent cytotoxicity against MCL cell lines^[3].
OSU-2S (2-8 μM; 24 h) induces apoptosis in MCL cell lines^[3].
OSU-2S (4-5 μM; 24 h) induces CD74 expression on the surface of MCL cells^[3].
OSU-2S (4 μM; 24 h) enhances the cytotoxicity of Milatuzumab (HY-P99731) against MCL cells by upregulating CD74^[3].
OSU-2S (2-10 μM; 48 h) demonstrates anti-proliferative activity against various HCC cell lines^[2].
OSU-2S (1.25-2.5 μM; 48 h) 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) enhances Sorafenib-induced apoptosis in HCC cells^[2].
OSU-2S (1.25-2.5 μM; 48 h) enhances the anti-HCC effect of Sorafenib via 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].
The activity of OSU-2S (1.25-7.5 μM) against HCC cells is influenced by p53 status; 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].

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) 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

CAS No. 1351056-65-9
Molecular Weight 335.52
Formula C₂₁H₃₇NO₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
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.

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

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

All PKC Isoforms