PKHB1
Based on 1 Customer Validation
PKHB1 (txCD47) is a CD47 agonist and Thrombospondin-1 peptide mimetic. PKHB1 activates CD47 and triggers Caspase-independent, calcium-dependent cell death via mitochondrial alterations, ROS production, endoplasmic reticulum morphological changes, and dissipation of mitochondrial membrane potential. PKHB1 induces the exposure of Calreticulin, HSP70, and HSP90, thereby driving immunogenic cell death. PKHB1 promotes intratumoral CD8+ T cell infiltration and inhibits breast tumorigenesis. PKHB1 reduces HSV-1 levels and alleviates the severity of herpes simplex keratitis. PKHB1 can be used in research related to breast cancer, herpes simplex keratitis, and T-cell acute lymphoblastic leukemia.
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- Pureza: 99.84%
- No. CAS: 1505523-99-8
- Fòrmula: C68H105N17O12S
- Peso molecular:1384.73
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Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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HSV-1 |
HSP70 |
HSP90 |
PKHB1 (100-400 μM; 2 h) induces concentration-dependent cell death in MCF-7, MDA-MB-231 and 4T1 breast cancer cells, with CC50 values of approximately 200 μM, 200 μM and 300 μM, respectively[1].
PKHB1 (200-300 μM; 2 h) induces loss of mitochondrial membrane potential, ROS production, and intracellular Ca2+ accumulation in MCF-7, MDA-MB-231, and 4T1 breast cancer cells at its CC50 concentration[1].
PKHB1 (200-300 μM; 2 h) induces the surface exposure of CALR, HSP70 and HSP90 on MCF-7, MDA-MB-231 and 4T1 breast cancer cells at its CC50 concentration[1].
The PKHB1 peptide (0-500 μM; 24 h) exhibits low cytotoxicity against HCECs, B4G12 cells, RAW264.7 cells, and THP1 cells[2].
At a concentration of 100 μM, the PKHB1 peptide does not directly inhibit HSV-1 replication in HSV-1-infected HCECs in the absence of immune cells[2].
PKHB1 (200 μM; 2 h) induces caspase-independent, calcium-dependent cell death and mitochondrial transmembrane potential loss in CCRF-CEM, MOLT-4 and L5178Y-R cells[3].
Incubation with PKHB1 (200-300 μM; 2 h) at the CC50 concentration for 2 hours across various cell lines induces significant calreticulin exposure on the surface of CCRF-CEM, MOLT-4 and L5178Y-R cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human corneal epithelial cells (HCECs), human corneal endothelial cells (B4G12), mouse monocyte-macrophage leukemia cells (RAW264.7), human myeloid leukemia mononuclear cells (THP-1)
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Concentration:0-500 μM (peptide treatment)
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Incubation Time:24 h (peptide treatment); 2 h (CCK-8 reagent)
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Result:Remained above 50% in B4G12 cells at 500 μM.
Showed CC50 values greater than 200 μM.
PKHB1 (200 µM; subconjunctival injection; 1 day before infection, 1 day after infection, 2 days after infection) prolongs the survival of mice with herpes simplex keratitis (HSK), reduces the replication level of HSV-1 in ocular tissues, alleviates the severity of HSK, and enhances the antiviral immune response by increasing the recruitment of antigen-presenting cells and CD8+ T cells[2].
PKHB1 (200 μg; intraperitoneal injection; once weekly for 6 consecutive weeks) induces complete tumor regression in L5178Y-R tumor-bearing BALB/c mice, restores white blood cell counts to healthy levels, and provides long-term anti-tumor protection, resulting in a 90% survival rate in mice after secondary challenge[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6- to 8-week-old, 22 g weight, subcutaneous inoculation of 5 × 105 live 4T1 cells)[1]
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Dosage:400 μg
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Administration:i.p.; daily
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Result:Reduced mean tumor volume to 570 mm3 (vs control 1500 mm3), achieving 62% tumor volume reduction.
Reduced mean tumor weight to 0.40 grams (vs control 1.5 grams), achieving 73% tumor weight reduction.
Increased percentage of CD3+ cells in blood, lymph nodes, and tumors.
Increased CD4+ cells in lymph nodes but decreased them in tumors.
Increased CD8+ T cells in peripheral blood and tumor sites but decreased them in lymph nodes.
Reduced blood MDSCs from 48% to 23%.
Reduced blood Tregs from 12% to 3%.
Increased CD8/Tregs ratio from 2% to 14%.
Induced 75% calcein-negative 4T1 cells in splenocyte co-culture (vs control 40%).
Chemical Information
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No. CAS 1505523-99-8
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Appearance Solid
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Peso molecular 1384.73
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Fòrmula C68H105N17O12S
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Color White to off-white
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Synonyms
txCD47
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Sequence
{d-Lys}-Arg-Phe-Tyr-Val-Val-Met-Trp-Lys-{d-Lys}
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Sequence Shortening
{d-Lys}-RFYVVMWK-{d-Lys}
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
H2O : ≥ 50 mg/mL (36.11 mM)
* "≥" means soluble, but saturation unknown.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Calvillo-Rodríguez KM, et al. PKHB1, a thrombospondin-1 peptide mimic, induces anti-tumor effect through immunogenic cell death induction in breast cancer cells. Oncoimmunology. 2022;11(1):2054305. Published 2022 Apr 4. [Content Brief]
[2]. He Y, et al. PKHB1 peptide induces antiviral effects through induction of immunogenic cell death in herpes simplex keratitis. Front Pharmacol. 2022;13:1048978. Published 2022 Dec 1. [Content Brief]
[3]. Uscanga-Palomeque AC, et al. CD47 agonist peptide PKHB1 induces immunogenic cell death in T-cell acute lymphoblastic leukemia cells. Cancer Sci. 2019;110(1):256-268. [Content Brief]
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). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.7222 mL | 3.6108 mL | 7.2216 mL | 18.0541 mL |
| 5 mM | 0.1444 mL | 0.7222 mL | 1.4443 mL | 3.6108 mL | |
| 10 mM | 0.0722 mL | 0.3611 mL | 0.7222 mL | 1.8054 mL | |
| 15 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 1.2036 mL | |
| 20 mM | 0.0361 mL | 0.1805 mL | 0.3611 mL | 0.9027 mL | |
| 25 mM | 0.0289 mL | 0.1444 mL | 0.2889 mL | 0.7222 mL | |
| 30 mM | 0.0241 mL | 0.1204 mL | 0.2407 mL | 0.6018 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PKHB1 Related Classifications
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