1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Transferrin Receptor Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase
  3. 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.

STIM1-TFR1-IN-1

STIM1-TFR1-IN-1 Chemical Structure

CAS No. : 2196106-61-1

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Description

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[1].

IC50 & Target[1]

TFR1

 

GPX4

 

In Vitro

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.

In Vivo

STIM1-TFR1-IN-1 (Compound S-IN-1) (10 mg/kg; p.o.; once every 24 h) significantly reduces brain tissue damage and continuously improves sensory, motor, and cognitive neurological deficits in a mouse model of intracerebral hemorrhage[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (adult male, 10-week-old, 20-25 g, intracerebral hemorrhage induced by autologous blood injection)[1]
Dosage: 10 mg/kg
Administration: p.o.; once every 24 h
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.
Molecular Weight

319.43

Formula

C15H21N5OS

CAS No.
SMILES

O=C(NC1=NN=C(C2CCC2)N1)[C@@H](N3C=CC=C3)CCSC

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

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
STIM1-TFR1-IN-1
Cat. No.:
HY-181953
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