SY-LB-57 is a potent bone morphogenetic protein (BMP) receptor signaling agonist and may be utilized in study/research of diseases like fractures and pulmonary hypertension.

Physicochemical Properties

Molecular Formula	C16H13N3O
Molecular Weight	263.293923139572
Exact Mass	263.105
CAS #	2253719-35-4
PubChem CID	164886644
Appearance	Off-white to light yellow solid powder
LogP	3.3
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	2
Heavy Atom Count	20
Complexity	351
Defined Atom Stereocenter Count	0
SMILES	C1(C2=CC3=C(N2)C=CC(OC)=C3)NC2=CC=CC=C2N=1
InChi Key	CKMZAHNTGUKLJF-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H13N3O/c1-20-11-6-7-12-10(8-11)9-15(17-12)16-18-13-4-2-3-5-14(13)19-16/h2-9,17H,1H3,(H,18,19)
Chemical Name	2-(5-methoxy-1H-indol-2-yl)-1H-benzimidazole
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	At a concentration less than 10 μM, SY-LB-57 (0.01-1000 μM, 24 h) can significantly induce cell proliferation in C2C12 cells, with an IC50 value of 807.93 μM [1]. In addition to promoting nuclear translocation of p-Smad and increasing Smad protein phosphorylation, SY-LB-57 (0.01-10 μM, 15-30 minutes) also activates the PI3K/Akt pathway and causes p-Akt to localize in the cytoplasm [1]. The cell cycle transition to proliferation can be induced by SY-LB-57 (0.01-10 μM, 24 h) [1].
Cell Assay	Cell Viability Determination[1] Cell Types: C2C12 Cell Tested Concentrations: 0.01-1000 μM Incubation Duration: 24 hrs (hours) Experimental Results: At 1 mM, C2C12 cell viability diminished by 85%, while cell viability increased by 280%, 290%, 200 0.01 μM, 0.1 %, 150% and 50% at µM, 1 µM, 10 µM and 100 µM respectively. Western Blot Analysis [1] Cell Types: C2C12 cells Tested Concentrations: 0.01-10 μM Incubation Duration: 15 minutes or 30 minutes Experimental Results: Smad protein phosphorylation increased Dramatically, 50% to 257% higher than the control after 30 minutes. demonstrated a significant increase in p-Akt expression levels, exceeding the control by 667-1081% after 15 minutes. Cell cycle analysis [1] Cell Types: C2C12 cells Tested Concentrations: 0.01-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: It resulted in a significant decrease in the percentage of cells in the G0/G1 phase and a significant increase in the cells in the S and G2/M phases.
References	[1]. Discovery of a novel class of benzimidazoles as highly effective agonists of bone morphogenetic protein (BMP) receptor signaling. Sci Rep. 2022 Jul 15;12(1):12146.

Solubility Data

Solubility (In Vitro)

DMSO : ~16.67 mg/mL (~63.31 mM)

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	3.7981 mL	18.9905 mL	37.9809 mL
	5 mM	0.7596 mL	3.7981 mL	7.5962 mL
	10 mM	0.3798 mL	1.8990 mL	3.7981 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.