Ceapin-A7 |
رقم الكتالوجGC61606
One-Click Copy Product Info
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سيابين-أ7 هو مانع انتقائي لإشارات ATF6α في الاستجابة للإجهاد ER، بتركيز قدره 0.59 ميكرومول/مل (IC50).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2323027-38-7
Sample solution is provided at 25 µL, 10mM.
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Ceapin-A7 is a selective blocker of endoplasmic reticulum stress ATF6α signaling (IC50= 0.59μM)[1]. Ceapin-A7 can inhibit Th17 cell differentiation[2]. Ceapin-A7 protects cells from Zika virus infection and also has the function of increasing the radiosensitivity of cancer cells[3-4].
In vitro, pretreatment of ccRCC cells (ACHN and 786-O) with Ceapin-A7 (20μM) for 24 hours reduced the protein expression of PINK1 and BNIP3, and promoted cell proliferation and migration[5]. Pretreatment of bovine pulmonary artery endothelial cells (BPAEC) with Ceapin-A7 (15μM) for 24 hours, followed by stimulation with LPS (1μg/ml) for 2 hours, significantly enhanced the phosphorylation activation of STAT3, JAK2, and JNK, while exacerbating the inhibition of cell proliferation[6].
In vivo, Ceapin-A7 (10mg/kg) was administered via intraperitoneal injection three times per week to DBA/1J mice with collagen-induced arthritis (CIA), from day 22 to day 45, Ceapin-A7 significantly alleviated arthritis severity and joint bone erosion[7]. Ceapin-A7 (1μM) was administered via drinking water to curdlan-induced SKG mice, from week 1 until week 12. Ceapin-A7 significantly alleviated spinal ankylosis and osteophyte formation[8].
References:
[1] Fakir S, Sigdel M, Sarker MMR, et al. Ceapin-A7 suppresses the protective effects of Octreotide in human and bovine lung endothelial cells. Cell Stress Chaperones. 2025 Feb;30(1):1-8.
[2] Kubra KT, Akhter MS, Saini Y, et al. Activating transcription factor 6 protects against endothelial barrier dysfunction. Cell Signal. 2022 Nov;99:110432.
[3] Kern J, Schilling D, Schneeweis C, et al. Identification of the unfolded protein response pathway as target for radiosensitization in pancreatic cancer. Radiother Oncol. 2024 Feb;191:110059.
[4] Mufrrih M, Chen B, Chan SW. Zika Virus Induces an Atypical Tripartite Unfolded Protein Response with Sustained Sensor and Transient Effector Activation and a Blunted BiP Response. mSphere. 2021 Jun 30;6(3):e0036121.
[5] Yan M, Wang J, Wang H, et al. Knockdown of NR3C1 inhibits the proliferation and migration of clear cell renal cell carcinoma through activating endoplasmic reticulum stress-mitophagy. J Transl Med. 2023 Oct 8;21(1):701.
[6] Kubra KT, Barabutis N. Ceapin-A7 potentiates lipopolysaccharide-induced endothelial injury. J Biochem Mol Toxicol. 2023 Nov;37(11):e23460.
[7] Ge L, Wang T, Shi D, et al. ATF6α contributes to rheumatoid arthritis by inducing inflammatory cytokine production and apoptosis resistance. Front Immunol. 2022 Oct 10;13:965708.
[8] Ma M, Li H, Wang P, et al. ATF6 aggravates angiogenesis-osteogenesis coupling during ankylosing spondylitis by mediating FGF2 expression in chondrocytes. iScience. 2021 Jun 28;24(7):102791.
| Cell experiment [1]: | |
Cell lines | ACHN and 786-O cells (human renal cell carcinoma cell lines) |
Preparation Method | ACHN and 786-O cells were maintained in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Ceapin-A7 at a concentration of 20μM for 5 hours. |
Reaction Conditions | 20μM; 5h |
Applications | Ceapin-A7 significantly down-regulated the expression of PINK1 and BNIP3 in NR3C1-knockdown ccRCC cells. Ceapin-A7 also reversed the increased LC3 expression and decreased P62 expression induced by NR3C1 knockdown, indicating inhibition of mitophagy. Additionally, Ceapin-A7 treatment rescued the reduced proliferation and migration capabilities of ccRCC cells caused by NR3C1 knockdown. |
| Animal experiment [2]: | |
Animal models | DBA/1J mice with collagen-induced arthritis (CIA) |
Preparation Method | CIA mice were intraperitoneally administered Ceapin-A7 (10mg/kg) three times per week from day 22 to day 45 post-immunization. Control groups received vehicle or etanercept (2mg/kg). |
Dosage form | 10mg/kg/day; i.p. |
Applications | Ceapin-A7 administration significantly reduced arthritis severity scores and paw swelling in CIA mice, comparable to etanercept treatment. Ceapin-A7 treatment decreased bone erosion parameters (Tb.Sp) while increasing bone mineral density (Tb.BMD) and trabecular number (Tb.N). Additionally, Ceapin-A7 reduced serum levels of inflammatory cytokines including IL-6, IL-8, TNF-α and IL-1β. Histological analysis showed Ceapin-A7 ameliorated synovial hyperplasia, pannus formation and cartilage destruction. |
References: | |
| Cas No. | 2323027-38-7 | SDF | |
| Canonical SMILES | O=C(NC1=CN(CC2=CC=C(C(F)(F)F)C=C2C(F)(F)F)N=C1)C3=NOC(C4=CC=CO4)=C3 | ||
| Formula | C20H12F6N4O3 | M.Wt | 470.32 |
| الذوبان | DMSO: 100 mg/mL (212.62 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1262 mL | 10.6311 mL | 21.2621 mL |
| 5 mM | 425.2 μL | 2.1262 mL | 4.2524 mL |
| 10 mM | 212.6 μL | 1.0631 mL | 2.1262 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)