STIM1-TFR1-IN-1
STIM1-TFR1-IN-1 is an orally active stromal interaction molecule 1 (STIM1)-transferrin receptor 1 (TFR1) protein complex inhibitor with a Kd of 2.18 μM for STIM1-CD protein. STIM1-TFR1-IN-1 blocks STIM1-TFR1 interaction and reduce TFR1-mediated iron uptake activity. STIM1-TFR1-IN-1 inhibits ferroptosis, lipid peroxidation and ROS production, enhances glutathione peroxidase 4 (GPX4) activity and glutathione/oxidized glutathione ratio, and rescues ferroptosis-associated mitochondrial morphological changes. STIM1-TFR1-IN-1 exhibits neuroprotective
effects and reduces brain injury. STIM1-TFR1-IN-1 can be used for the research of intracerebral hemorrhage.
For research use only. We do not sell to patients.
- CAS No.: 2196106-61-1
- Formula: C15H21N5OS
- Molecular Weight:319.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
effects and reduces brain injury. STIM1-TFR1-IN-1 can be used for the research of intracerebral hemorrhage[1].
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TFR1 |
GPX4 |
STIM1-TFR1-IN-1 (Compound S-IN-1) (0.15625-5 μM) directly and specifically binds to the STIM1-CD protein with a Kd of 2.18 μM[1].
S-IN-1 (10-20 μM) inhibits the interaction between STIM1 and TFR1 in HT22 mouse neuronal cells exposed to Hemin (HY-19424) to model ICH[1].
S-IN-1 (0-40 μM) attenuates neuronal ferroptosis and increases the vitality of neuronal cells in Hemin-treated HT22 mouse neuronal cells by reducing iron accumulation, lipid peroxidation, and ROS, while enhancing antioxidant defense system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (adult male, 10-week-old, 20-25 g, intracerebral hemorrhage induced by autologous blood injection)[1]
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Dosage:10 mg/kg
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Administration:p.o.; once every 24 h
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Result:Reduced brain edema, increased the number of surviving neurons, and lowered plasma neuron-specific enolase (NSE) levels on day 3 post-ICH.
Significantly improved modified neurological severity score (mNSS), corner test scores, cylinder test scores, adhesive removal time, and rotarod fall latency on day 3 post-ICH.
Continuously improved mNSS, corner test scores, cylinder test scores, adhesive removal time, rotarod fall latency, novel object location (NOL) discrimination ratios, and novel object recognition (NOR) discrimination ratios over 14 days post-ICH compared to vehicle controls.
Chemical Information
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CAS No. 2196106-61-1
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Molecular Weight 319.43
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Formula C15H21N5OS
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SMILES
O=C(NC1=NN=C(C2CCC2)N1)[C@@H](N3C=CC=C3)CCSC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STIM1-TFR1-IN-1 Related Classifications
HY-181953 Related Classifications
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- STIM1-TFR1-IN-1
- 2196106-61-1
- Transferrin Receptor
- Ferroptosis
- Reactive Oxygen Species (ROS)
- Glutathione Peroxidase
- STIM1-TFR1 protein complex
- reactive oxygen species
- ferroptosis
- glutathione peroxidase 4
- STIM1
- iron uptake activity
- Lys385 site
- lipid peroxidation
- neuronal iron accumulation
- TFR1
- Inhibitor
- inhibitor
- inhibit