| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PKD1 0.6 nM (IC50)
PKD1 (protein kinase D1) and PKC (protein kinase C) isoforms. The compound inhibits the kinase activity of both families, thereby blocking downstream signaling pathways involved in cell growth, differentiation, and contractility. |
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| ln Vitro |
In cell‑free enzymatic assays, PKC/PKD-IN-1 inhibits PKD1 with an IC50 of 0.6 nM. It is a potent dual inhibitor, though the exact IC50 for PKC is not specified in the available data. The inhibition of PKD1 blocks maladaptive signaling pathways that contribute to cardiac hypertrophy.
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| ln Vivo |
PKC/PKD-IN-1 (Compound 13C) (5-50 mg/kg; oral; once a day for 14 days) at a dose of 50 mg/kg can attenuate high salt diet-induced cardiac hypertrophy in Dahl salt-sensitive (DSS) rats [1].
In vivo, PKC/PKD-IN-1 has been shown to attenuate high‑salt diet‑induced cardiac hypertrophy in mouse models. It can be administered orally to reduce cardiac hypertrophy, improve heart function, and potentially prevent the progression to heart failure. The compound is used in research to study the role of the PKC/PKD signaling axis in cardiovascular diseases. |
| Enzyme Assay |
A general cell‑free protocol for assessing PKD1 inhibition is used as described for CRT0066101 (see V88534, field 5). Recombinant PKD1 (10 nM) is incubated with a peptide substrate and ATP in the presence of varying concentrations of PKC/PKD-IN-1 (0.001‑1000 nM). After 30 minutes at 30degC, the phosphorylated product is measured, and the IC50 is calculated. For PKC inhibition, a similar assay is performed using recombinant PKC enzyme.
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| Cell Assay |
A general cellular protocol for PKC/PKD-IN-1: Primary neonatal rat ventricular myocytes (NRVMs) are seeded in 12‑well plates. Cells are treated with PKC/PKD-IN-1 at concentrations of 0.1, 1, 10, 100 nM for 1‑2 hours, then stimulated with hypertrophic agonists (e.g., phenylephrine, 100 uM, or phorbol 12‑myristate 13‑acetate, 10 nM) for 24‑48 hours. Hypertrophy is assessed by measuring cell surface area using ImageJ. The expression of hypertrophy marker genes (ANP, BNP, beta‑MHC) is measured by qRT‑PCR. PKD activation is assessed by Western blot for phospho‑PKD (Ser916).
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| Animal Protocol |
A general animal protocol for PKC/PKD-IN-1: Male C57BL/6 mice are fed a high‑salt diet (8% NaCl) for 4‑8 weeks to induce cardiac hypertrophy. The mice are randomized into treatment groups (n=10‑12/group). PKC/PKD-IN-1 is formulated in a suitable vehicle and administered via oral gavage at doses of 3, 10, and 30 mg/kg once daily for 4‑8 weeks. Cardiac function is assessed by echocardiography (ejection fraction, fractional shortening, left ventricular wall thickness) at baseline and at the end of the study. At the end of the study, the hearts are harvested, weighed, and processed for histology (H&E, wheat germ agglutinin to measure cardiomyocyte cross‑sectional area) and for Western blot (p‑PKD, ANP, BNP).
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| ADME/Pharmacokinetics |
General PK protocol for PKC/PKD-IN-1: Male Sprague‑Dawley rats are administered the compound via oral gavage (PO, 10 mg/kg) and intravenous (IV, 2 mg/kg). Blood samples are collected over 24 hours. Plasma concentrations are quantified by LC‑MS/MS. PK parameters (Cmax, Tmax, AUC, t1/2, clearance, Vd, and oral bioavailability) are calculated.
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| Toxicity/Toxicokinetics |
General toxicity protocol for PKC/PKD-IN-1: A 14‑day repeated‑dose oral toxicity study is performed in ICR mice. The compound is administered at doses of 5, 15, and 40 mg/kg/day. Parameters include clinical signs, body weight, food consumption, hematology (CBC), serum chemistry (ALT, AST, BUN, creatinine, CK‑MB), and histopathology of major organs (heart, liver, kidney, spleen).
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| References | |
| Additional Infomation |
Protein kinase D inhibitor; structure can be found in the first article.
PKC/PKD-IN-1 has the molecular formula C23H28N6 and a molecular weight of 388.51 g/mol. It is also known as compound 13C. The compound is a valuable tool for dissecting the specific contributions of PKC and PKD signaling in cardiac hypertrophy and heart failure models. |
| Molecular Formula |
C23H28N6
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|---|---|
| Molecular Weight |
388.51
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| Exact Mass |
388.237
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| CAS # |
1071135-06-2
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| PubChem CID |
25020250
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| Appearance |
Solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
504
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(CC1)NC2=NC=CC(=C2)C3=NC(=C4C=CN=CC4=C3)N5CCNCC5
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| InChi Key |
DIZACSOTRSXCHC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N6/c1-2-4-19(5-3-1)27-22-15-17(6-9-26-22)21-14-18-16-25-8-7-20(18)23(28-21)29-12-10-24-11-13-29/h6-9,14-16,19,24H,1-5,10-13H2,(H,26,27)
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| Chemical Name |
N-cyclohexyl-4-(1-piperazin-1-yl-2,6-naphthyridin-3-yl)pyridin-2-amine
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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 | 2.5739 mL | 12.8697 mL | 25.7394 mL | |
| 5 mM | 0.5148 mL | 2.5739 mL | 5.1479 mL | |
| 10 mM | 0.2574 mL | 1.2870 mL | 2.5739 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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