JBSNF-000028 hydrochloride
Based on 1 Customer Validation
JBSNF-00002 hydrochloride is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 hydrochloride can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 hydrochloride exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 hydrochloride can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease.
For research use only. We do not sell to patients.
- Purity : 95.64%
- Formula: C11H14ClN3
- Molecular Weight:223.70
-
Storage:
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)
Biological Activity
Description
IC50 & Target
IC50: 0.033 μM (hNNMT), 0.19 μM (mkNNMT), 0.21 μM (mNNMT)[1]
In Vitro
JBSNF-000028 hydrochloride (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells[1].
JBSNF-000028 hydrochloride (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells[1].
JBSNF-000028 hydrochloride binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain)[1].
JBSNF-000028 hydrochloride is inactive against a broad panel of targets related to metabolism and safety[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
JBSNF-000028 hydrochloride (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Appearance Solid
-
Molecular Weight 223.70
-
Formula C11H14ClN3
-
Color Off-white to light yellow
-
SMILES
CN1CC2=C3C(CCN3C1=N)=CC=C2.Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
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)
Solvent & Solubility
In Vitro:
DMSO : 16.67 mg/mL (74.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4703 mL | 22.3514 mL | 44.7027 mL | 111.7568 mL |
| 5 mM | 0.8941 mL | 4.4703 mL | 8.9405 mL | 22.3514 mL | |
| 10 mM | 0.4470 mL | 2.2351 mL | 4.4703 mL | 11.1757 mL | |
| 15 mM | 0.2980 mL | 1.4901 mL | 2.9802 mL | 7.4505 mL | |
| 20 mM | 0.2235 mL | 1.1176 mL | 2.2351 mL | 5.5878 mL | |
| 25 mM | 0.1788 mL | 0.8941 mL | 1.7881 mL | 4.4703 mL | |
| 30 mM | 0.1490 mL | 0.7450 mL | 1.4901 mL | 3.7252 mL | |
| 40 mM | 0.1118 mL | 0.5588 mL | 1.1176 mL | 2.7939 mL | |
| 50 mM | 0.0894 mL | 0.4470 mL | 0.8941 mL | 2.2351 mL | |
| 60 mM | 0.0745 mL | 0.3725 mL | 0.7450 mL | 1.8626 mL |