OSU-2S is a potent PKCδ activator. OSU-2S inhibits cell growth/proliferation and migration. When combined with Sorafenib, the expression of p-ERK1/2 is reduced and the expression of PKCδ (38 kDa) is increased. OSU-2S causes apoptosis (Apoptosis). OSU-2S slao is a non-immunosuppressive analog of FTY720. OSU-2S has anti-cancer effect.

Physicochemical Properties

Molecular Formula	C21H38CLNO2
Molecular Weight	371.984925746918
Exact Mass	371.259
CAS #	1351056-65-9
Related CAS #	1351056-65-9;
PubChem CID	53234284
Appearance	Typically exists as solid at room temperature
LogP	5.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	13
Heavy Atom Count	24
Complexity	300
Defined Atom Stereocenter Count	1
SMILES	CCC[C@](CCC1=CC=C(C=C1)OCCCCCC(C)C)(CO)N
InChi Key	MDUCYXCGWGNEMH-NRFANRHFSA-N
InChi Code	InChI=1S/C21H37NO2/c1-4-14-21(22,17-23)15-13-19-9-11-20(12-10-19)24-16-7-5-6-8-18(2)3/h9-12,18,23H,4-8,13-17,22H2,1-3H3/t21-/m0/s1
Chemical Name	(2S)-2-amino-2-[2-[4-(6-methylheptoxy)phenyl]ethyl]pentan-1-ol
Synonyms	OSU-2S Hydrochloride; OSU 2S Hydrochloride; OSU2S Hydrochloride
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	When coupled with Sorafenib (2.5, 5 µM), OSU-2S (1.25, 2.5 µM; 48 h) decreases the expression of p-ERK1/2 and enhances the expression of PKCδ (38 kDa) [1]. OSU-2S/Sorafenib (OSU-2S 0.25, 2.5 µM; 8 h) combination inhibits cell motility and migration[1]. It decreases PARP expression in Hep3B cells in a dose- and time-regulated manner. Hep3B cells are induced by OSU-2S (5 µM; 12, 24 h) [2]. Hep3B, Huh7, and PLC-5 are stimulated in a dose-dependent manner by OSU-2S (0-10 µM; 1 h).
ln Vivo	Tumor growth is inhibited by OSU-2S (5, 10 mg/kg; ip; once daily for 42 days) [2].
Cell Assay	Cell proliferation assay[1] Cell Types: Hep3B, Huh7, PLC-5, HepG2 Cell Tested Concentrations: 0-10 µM Incubation Duration: 48 h Experimental Results: demonstrated anti-proliferative effect with IC50 of 2.53 Hep3B, Huh7, PLC-5, HepG2 cells were, 2.41, 3.96, and 1.84 µM respectively. Western Blot Analysis[1] Cell Types: Hep3B Cell Tested Concentrations: 1.25, 2.5 µM Combined incubation time with sorafenib (2.5, 5 µM): 48 h Experimental Results: diminished ERK1/2 phosphorylated expression, PKCδ (38 kDa) expression increased) when combined with sorafenib/OSU-2S.
Animal Protocol	Animal/Disease Models: CD2F1 mice (Hep3B tumor xenograft model) [2] Doses: 5, 10 mg/kg Route of Administration: IP; one time/day for 42 days Experimental Results: Demonstrated higher tumor suppressor potency, bioluminescence at end of treatment 80% reduction.
References	[1]. OSU-2S/Sorafenib Synergistic Antitumor Combination against Hepatocellular Carcinoma: The Role of PKCδ/p53. Front Pharmacol. 2016 Nov 30;7:463. [2]. Antitumor effects of OSU-2S, a nonimmunosuppressive analogue of FTY720, in hepatocellular carcinoma. Hepatology. 2011 Jun;53(6):1943-58.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6883 mL	13.4416 mL	26.8832 mL
	5 mM	0.5377 mL	2.6883 mL	5.3766 mL
	10 mM	0.2688 mL	1.3442 mL	2.6883 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.