Cyproheptadine hydrochloride
Based on 6 publication(s) in Google Scholar
Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 969-33-5
- Formula: C21H22ClN
- Molecular Weight:323.86
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Cyproheptadine hydrochloride
MoreAll Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
Chk2 |
CDK1 |
CDK2 |
CDK3 |
Cyproheptadine (0-30 μM; 3-24 h) hydrochloride reduces cyclin D1, D2, and D3 protein and mRNA levels in human multiple myeloma (LP-1, KMS11, OCI-MY5, U266, MM1.R, OPM1, KMS12) and leukemia (OCI-AML2, OCI-AML3, HL60, OCI-M2, NB4, Jurkat) cell lines in a time- and concentration-dependent manner[2].
Cyproheptadine (0-20 μM) hydrochloride arrests human multiple myeloma (LP-1, MM1.S, MM1.R, KMS11) and leukemia (OCI-AML2, Jurkat) cell lines in the G0/G1 phase, reduces cellular proliferation, increases p21 expression, and decreases AP2A expression in a time- and concentration-dependent manner[2].
Cyproheptadine (0-30 μM; 24-72 h; 7-14 days) hydrochloride reduces viability and induces apoptosis in human multiple myeloma and leukemia cell lines and primary patient samples, inhibits clonogenic growth of primary AML samples, and exhibits reduced toxicity toward normal human hematopoietic stem cells, with cytotoxic effects occurring in a time- and concentration-dependent manner[2].
Cyproheptadine (0-30 μM; 24-48 h) hydrochloride induces caspase-dependent apoptosis in human multiple myeloma (OCI-MY5, OPM1, U266, LP-1) and leukemia (OCI-AML2, CEM, NB4) cell lines and murine leukemia (MDAY-D2) cells via activation of the mitochondrial pathway of caspase activation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and Huh-7 cells
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Concentration:20, 40, 60, 80, 100, 120 μM
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Incubation Time:24 h
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Result:Inhibited cell proliferation in a dose-dependent manner.
Showed IC50 of 44.4 and 44.7 μM in HepG2 cells and Huh-7 cells, respectively.
Cyproheptadine (10 mg/kg; i.p.; once daily; for 10 consecutive days) hydrochloride reduces the expression level of Cyclin D2 protein in a subcutaneous multiple myeloma xenograft model[2].
Cyproheptadine (10 mg/kg; i.p.; once daily; for 5 consecutive days) hydrochloride reduces the protein expression levels of cyclin D2 and cyclin D3 in subcutaneous leukemia xenograft models[2].
Cyproheptadine (40 mg/kg; i.p.; once daily for 7 consecutive days) hydrochloride completely eliminates malignant ascites formation in a mouse intraperitoneal leukemia model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (sublethally irradiated with 3.5 Gy)[2]
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Dosage:36 mg/kg
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Administration:i.p.; daily; 7 weeks
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Result:Delayed tumor growth, resulting in an approximately 2-fold reduction in tumor volume at the end of the 7-week treatment period.
Showed statistical significance at 35 days (P = .048) and 49 days (P = .032) post-treatment initiation.
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Animal Model:NOD/SCID (sublethally irradiated with 3.5 Gy)[2]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Decreased cyclin D2 protein expression in xenografted LP-1 tumors compared to vehicle control tumors, as detected by immunoblotting.
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Animal Model:NOD/SCID (sublethally irradiated with 3.5 Gy)[2]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 5 days
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Result:Decreased cyclin D2 and cyclin D3 protein expression in xenografted MDAY-D2 tumors compared to vehicle control tumors, as detected by immunoblotting.
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Animal Model:DBA2[2]
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Dosage:40 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Completely abolished formation of malignant ascites; no measurable ascites volume or malignant cell count was detected in treated mice, compared to vehicle control mice with median ascites volume of ~3 mL and median ascites cell count of ~1×108 cells.
Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Cyproheptadine hydrochloride is primarily used to establish a rat model of reversible diabetes-like conditions or β-cell functional inhibition, characterized by non-fasting hyperglycemia, abnormal glucose tolerance, reduced pancreatic insulin levels, and abnormal β-cell morphology[3].
Administration: Cyproheptadine hydrochloride (22.5-90 mg/kg): administered orally once daily for 14 days.
Histology analysis: Vacuolization of islet tissue; vesiculation of the rough endoplasmic reticulum and loss of secretory granules in β-cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 969-33-5
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Appearance Solid
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Molecular Weight 323.86
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Formula C21H22ClN
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Color White to off-white
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SMILES
CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24.Cl
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Synonyms
Cyproheptadine HCl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Glia
Sustained Neuronal Stimulation Activates Paraventricular Thalamus Astrocytes for Chronicity of Neuropathic Pain in Mice. [Abstract]2026 Aug;74(8):e70183. PMID: 42231639 -
Front Pharmacol
Prediction of Synergistic Drug Combinations for Prostate Cancer by Transcriptomic and Network Characteristics. [Abstract]2021 Apr 12;12:634097. PMID: 33986671 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
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Cureus
2023 Nov 27;15(11):e49530. PMID: 38033435 -
Cureus
2023 Nov 27;15(11):e49530. PMID: 38033435
Solvent & Solubility
DMSO : 50 mg/mL (154.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (306 KB)
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SDS (585 KB)
- English - EN (585 KB)
- Français - FR (585 KB)
- Deutsch - DE (585 KB)
- Norwegian - NO (585 KB)
- Español - ES (585 KB)
- Swedish - SV (585 KB)
- Italian - IT (585 KB)
- Korean - KR (585 KB)
- Portuguese - PT (585 KB)
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Handling Instructions (2659 KB)
References
[1]. Feng YM, et al. Cyproheptadine, an antihistaminic drug, inhibits proliferation of hepatocellular carcinoma cells by blocking cell cycle progression through the activation of P38 MAP kinase. BMC Cancer. 2015;15:134. Published 2015 Mar 17. [Content Brief]
[2]. Mao X, et al. Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008;112(3):760-769. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0878 mL | 15.4388 mL | 30.8775 mL | 77.1939 mL |
| 5 mM | 0.6176 mL | 3.0878 mL | 6.1755 mL | 15.4388 mL | |
| 10 mM | 0.3088 mL | 1.5439 mL | 3.0878 mL | 7.7194 mL | |
| 15 mM | 0.2059 mL | 1.0293 mL | 2.0585 mL | 5.1463 mL | |
| 20 mM | 0.1544 mL | 0.7719 mL | 1.5439 mL | 3.8597 mL | |
| 25 mM | 0.1235 mL | 0.6176 mL | 1.2351 mL | 3.0878 mL | |
| 30 mM | 0.1029 mL | 0.5146 mL | 1.0293 mL | 2.5731 mL | |
| 40 mM | 0.0772 mL | 0.3860 mL | 0.7719 mL | 1.9298 mL | |
| 50 mM | 0.0618 mL | 0.3088 mL | 0.6176 mL | 1.5439 mL | |
| 60 mM | 0.0515 mL | 0.2573 mL | 0.5146 mL | 1.2866 mL | |
| 80 mM | 0.0386 mL | 0.1930 mL | 0.3860 mL | 0.9649 mL | |
| 100 mM | 0.0309 mL | 0.1544 mL | 0.3088 mL | 0.7719 mL |
Cyproheptadine hydrochloride Related Classifications
HY-B0366A Related Classifications
Powered by Bioz
- Cyproheptadine
- 969-33-5
- Cyproheptadine HCl
- p38 MAPK
- Checkpoint Kinase (Chk)
- Histamine Receptor
- 5-HT Receptor
- CDK
- PARP
- Apoptosis
- CHK2
- histamine H1 receptor
- LP-1
- hepatocellular carcinoma
- acute myeloid leukemia
- human hematopoietic stem cells
- p38 MAP kinase
- serotonin receptor
- multiple myeloma
- MDAY-D2 cells
- Inhibitor
- inhibitor
- inhibit