CaMKII-IN-1 |
Catalog No.GC35601
One-Click Copy Product Info
|
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with an IC50 value of 63nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1208123-85-6
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with an IC50 value of 63nM [1]. CaMKII-IN-1 can inhibit the phosphorylation of CaMKII, p38 and Jnk, reduce the basal expression levels of MMP2, MMP9 and MCP1, as well as the expression level of Ang II, and prevent cell apoptosis by inhibiting the upregulation of Bax and cleaved caspase-3[2]. CAMKII-IN-1 has been widely used to inhibit the biosynthesis of Juvenile hormone (JH) and regulate the interaction between CREB and CBP[3].
In vitro, CAMKII-IN-1 treatment (40nM) for 48 hours reversed the elevated levels of p-CaMKII and p-Akt proteins in deES-2 cells with overexpressed CACNA1H, restoring the protein levels of LC3-II/LC3-I and Beclin1[4]. Treatment with 100nM CAMKII-IN-1 for 48 hours prevented the upregulation of Il17d expression in MC38 cells induced by WNT11, and reversed the increase in NF-κB p65 nuclear translocation induced by WNT11[5]. The 1-hour pre-treatment with CAMKII-IN-1 (100nM) significantly inhibited the upregulation of TGFα in BV2 cells after glibenclamide treatment[6]. The treatment with CAMKII-IN-1 (30nM) for 72 hours significantly promoted the proliferation of IEC-6 cells after serum deprivation[7].
In vivo, CAMKII-IN-1 treatment via microinjection into the nucleus accumbens shell (NAcsh) at a single dose of 63nM (1μl per side) rescued the stress sensitivity induced by LV-shPRCP in mice subjected to sub-threshold social defeat stress (SSDS), including an increase in social interaction rate and a reduction in inactivity time[8].
References:
[1] Asano S, Komiya M, Koike N, et al. 5, 6, 7, 8-Tetrahydropyrido [4, 3-d] pyrimidines as novel class of potent and highly selective CaMKII inhibitors[J]. Bioorganic & medicinal chemistry letters, 2010, 20(22): 6696-6698.
[2] Xu C, Xu J, Zou C, et al. Chronic Intermittent Hypoxia Regulates CaMKII‐Dependent MAPK Signaling to Promote the Initiation of Abdominal Aortic Aneurysm[J]. Oxidative Medicine and Cellular Longevity, 2021, 2021(1): 2502324.
[3] Zhu S, Liu F, Chen X, et al. Inter-organelle communication dynamically orchestrates juvenile hormone biosynthesis and female reproduction[J]. National Science Review, 2025, 12(3): nwaf022.
[4] Shi H, Zheng L, Jiang X, et al. CACNA1H restrains chemotherapy resistance in ovarian clear cell carcinoma cells by repressing autophagy[J]. Molecular Genetics and Genomics, 2024, 299(1): 77.
[5] Jiang W, Guan B, Sun H, et al. WNT11 promotes immune evasion and resistance to Anti-PD-1 therapy in liver metastasis[J]. Nature Communications, 2025, 16(1): 1429.
[6] He Y, Peng Y, Chang Y, et al. Blocking SUR1-TRPM4 reduces neuronal loss in peri-infarct area via stimulating TGFα released by microglia[J]. 2022.
[7] Lei X, Xu Z, Liu X, et al. Melatonin Influences Bmi1+ Intestinal Stem Cell Fate Through Metabolic Regulation After Irradiation[J]. Journal of Pineal Research, 2026, 78(1): e70110.
[8] Deng Q, Zhang S, Yang P, et al. α-MSH-catabolic enzyme prolylcarboxypeptidase in nucleus accumbens shell ameliorates stress susceptibility in mice through regulating synaptic plasticity[J]. Acta Pharmacologica Sinica, 2023, 44(8): 1576-1588.
| Cell experiment [1]: | |
Cell lines | IEC-6 cells |
Preparation Method | IEC-6 cells were seeded at a density of 5×103 cells/well in a 96-well plate and cultured in DMEM medium supplemented with 1% FBS and 1% penicillin and streptomycin for 12h. IEC-6 cells were subsequently cultured in FBS-free DMEM supplemented with 1% penicillin and streptomycin for 24h. After nutrient deprivation, the IEC-6 cells were treated with vehicle, melatonin (25μM), a selective chelator for calcium, BAPTA (1μM), the CaMKII-IN-1 (30nM), the selective DRP1 inhibitor Mdivi-1 (1μM), or the ROS inhibitor acetylcysteine for 72h. Cell viability was analyzed. |
Reaction Conditions | 30nM; 72h |
Applications | CaMKII-IN-1 treatment significantly enhanced cell proliferation of IEC-6 cells after serum deprivation. |
References: | |
| Cas No. | 1208123-85-6 | SDF | |
| Canonical SMILES | O=S(C1=CC=CC(Cl)=C1C)(NC2=C(CN(CC3=CC=CC=C3)CC4)C4=NC(NCCC5=CC=CC=C5)=N2)=O | ||
| Formula | C29H30ClN5O2S | M.Wt | 548.1 |
| Solubility | DMSO: ≥ 54 mg/mL (98.52 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8245 mL | 9.1224 mL | 18.2448 mL |
| 5 mM | 364.9 μL | 1.8245 mL | 3.649 mL |
| 10 mM | 182.4 μL | 912.2 μL | 1.8245 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)