| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
CJJ-300 targets the TGF-β receptor complex, specifically disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex. This places the compound within the TGF-β/Smad signaling pathway. By preventing the assembly of the active receptor complex, CJJ-300 inhibits downstream signaling events including the phosphorylation of Smad2 and Smad3 (P-Smad2/Smad3). The compound also attenuates TGF-β-induced phosphorylation of Erk1/2 and Akt, indicating broader modulation of TGF-β-mediated signaling cascades. Its mechanism involves protein-protein interaction inhibition rather than direct kinase inhibition.
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| ln Vitro |
CJJ300 inhibits TGF-β receptor dimerization (IC50 = 23.6 ± 5.8 µM) and tampers with protein-protein interactions[1]. Without causing cytotoxicity, CJJ300 (0-80 µM, 2 h) suppresses the expression of EMT (epithelial-mesenchymal transition) markers and the phosphorylation of intracellular mediators in the downstream TGF-β signaling pathway [1]. The TGF-β-induced cell migration is inhibited by CJJ300 [1].
In vitro, CJJ-300 inhibits TGF-β receptor dimerization with an IC₅₀ of 23.6 ± 5.8 µM and disrupts protein-protein interactions. At concentrations ranging from 0-80 µM over 2 hours, CJJ-300 suppresses the expression of EMT markers such as fibronectin, α-SMA, and MMP-2 in a dose-dependent manner without causing cytotoxicity. The compound inhibits TGF-β-induced cell migration. Western blot analysis in human A549 lung epithelial cells treated with 20, 40, and 80 µM CJJ-300 for 2 hours shows dramatic attenuation of TGF-β-induced increases in P-Smad2/Smad3, P-Erk1/2, and P-Akt. |
| ln Vivo |
In vivo activity data for CJJ-300 are limited as the compound is primarily characterized in vitro. As a TGF-β signaling inhibitor, the compound is expected to modulate TGF-β-mediated processes such as fibrosis, immune suppression, and tumor progression in animal models. The lack of reported cytotoxicity at concentrations up to 80 µM suggests favorable tolerability in vitro. Further in vivo studies would be required to assess the compound's efficacy in disease models such as pulmonary fibrosis, renal fibrosis, or cancer metastasis where TGF-β signaling plays a pathogenic role.
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| Enzyme Assay |
CJJ-300 is evaluated in vitro for its ability to inhibit TGF-β receptor dimerization and downstream signaling. Typical protocols involve cell-based assays using TGF-β-responsive reporter systems or western blot analysis of phosphorylated Smad proteins. Human A549 lung epithelial cells are treated with CJJ-300 at concentrations of 20, 40, and 80 µM for 2 hours prior to TGF-β stimulation. Receptor dimerization assays measure the formation of the TGF-β-TβR-I-TβR-II complex using immunoprecipitation or proximity ligation assays. IC₅₀ values for receptor dimerization inhibition are calculated from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human A549 Lung Epithelial Cells Tested Concentrations: 20, 40 and 80 µM Incubation Duration: 2 hrs (hours) Experimental Results: Increases in P-Smad2/Smad3, P-Erk1/2 and P-Akt were Dramatically attenuated by TGF-β induction. Downregulates the expression of EMT-related proteins, including fibronectin, α-SMA, and MMP-2, in a dose-dependent manner. Cell-based assays for CJJ-300 are conducted in human A549 lung epithelial cells. Cells are seeded in culture plates and treated with CJJ-300 at concentrations of 20, 40, and 80 µM for 2 hours, followed by stimulation with TGF-β. Protein lysates are collected and analyzed by western blot for EMT markers (fibronectin, α-SMA, MMP-2) and phosphorylated signaling proteins (P-Smad2/Smad3, P-Erk1/2, P-Akt). Cell migration is assessed using wound healing or transwell migration assays. Cytotoxicity is evaluated using standard viability assays to confirm that observed effects are not due to general toxicity. |
| Animal Protocol |
In vivo animal studies for CJJ-300 have not been extensively reported in the available literature. For TGF-β inhibitors in general, animal models include bleomycin-induced pulmonary fibrosis in mice, unilateral ureteral obstruction for renal fibrosis, and xenograft or syngeneic tumor models for cancer research. Typical protocols involve oral or intraperitoneal administration of the compound, with endpoints including tissue histology, fibrosis scoring, and analysis of phosphorylated Smad and EMT marker expression by immunohistochemistry or western blot. CJJ-300's efficacy in such models would require further investigation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CJJ-300 are not extensively reported in the available literature. As a small molecule with a molecular weight of 435.60 g/mol and high lipophilicity (LogP 7.5), the compound is expected to have moderate to high plasma protein binding and extensive tissue distribution. Typical PK parameters for similar TGF-β inhibitors include oral bioavailability, clearance, and half-life determined by LC-MS/MS analysis. The compound should be stored as a powder at -20°C for 3 years or 4°C for 2 years, and in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
CJJ-300 is supplied for research use only and is not intended for human administration. Toxicity data are limited, but the compound shows no cytotoxicity at concentrations up to 80 µM in human A549 lung epithelial cells. General laboratory safety precautions should be followed when handling. The compound is a TGF-β signaling inhibitor that blocks receptor complex formation. No specific toxicological studies have been published. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
CJJ-300 (CAS 1807631-83-9) is a research compound supplied for laboratory use only. It is not an approved drug and has no clinical trial or marketing authorization status. The compound is a TGF-β inhibitor that disrupts the TGF-β-TβR-I-TβR-II signaling complex with an IC₅₀ of 5.3 µM. It is available in research-grade purity (≥98%). The compound has three hydrogen bond donors, three acceptors, and nine rotatable bonds. It is typically stored as a white to off-white solid powder at -20°C or 4°C.
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| Molecular Formula |
C30H33N3
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| Molecular Weight |
435.603127241135
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| Exact Mass |
435.267
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| CAS # |
1807631-83-9
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| PubChem CID |
122211714
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| Appearance |
White to off-white solid powder
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| LogP |
7.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
439
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C(=C(C(=C(C=1C)CNC1C=CC=CC=1)C)CNC1C=CC=CC=1)C)NC1C=CC=CC=1
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| InChi Key |
AKBFUAPLAQSPMJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H33N3/c1-22-28(19-31-25-13-7-4-8-14-25)23(2)30(21-33-27-17-11-6-12-18-27)24(3)29(22)20-32-26-15-9-5-10-16-26/h4-18,31-33H,19-21H2,1-3H3
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| Chemical Name |
N-[[3,5-bis(anilinomethyl)-2,4,6-trimethylphenyl]methyl]aniline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2957 mL | 11.4784 mL | 22.9568 mL | |
| 5 mM | 0.4591 mL | 2.2957 mL | 4.5914 mL | |
| 10 mM | 0.2296 mL | 1.1478 mL | 2.2957 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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