| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ABHD16A (α/β-hydrolase domain-containing protein 16A). ABHD16A is a phosphatidylserine lipase that generates lyso-PS in mammalian cells. The target is involved in immunomodulatory signaling pathways.
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| ln Vitro |
KC01 (0-20 μM; 30 min) is an ABHD16A that may be active, with an IC50 of less than 90 nM[1]. Lyso-PSs of carriers COL205, K562, and MCF7 can be greatly reduced by KC01 (1 μM; 4 h). In mouse giant cells, KC01 (1 μM; 4 h) can also diminish lyso-PS and lipopolysaccharide-induced cytokine production[1].
KC01 inhibits human ABHD16A (hABHD16A) with an IC50 of 90 nM and mouse ABHD16A (mABHD16A) with an IC50 of 520 nM. KC01 (1 µM, 4 h) significantly reduces lyso-PSs in colon cancer cells (COL205, K562, and MCF7). KC01 (1 µM, 4 h) reduces lyso-PS and LPS-induced cytokine production in mouse macrophages. |
| ln Vivo |
KC01 significantly reduces lyso-PSs and decreases lyso-PS and LPS-induced cytokine production in mouse macrophages. It can deplete lysoPSs from cells, including lymphoblasts derived from subjects with PHARC. Detailed in vivo activity data in animal models has not been extensively reported in the available literature.
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| Enzyme Assay |
ABHD16A enzymatic activity assay: Recombinant human or mouse ABHD16A is incubated with varying concentrations of KC01 and a fluorogenic substrate (e.g., a phosphatidylserine analogue or p-nitrophenyl ester) in assay buffer (50 mM HEPES pH 7.4, 150 mM NaCl, 1 mM DTT, 0.01% Triton X-100) at 37°C for 30-60 min. The reaction is terminated and fluorescence or absorbance is measured. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T Tested Concentrations: 0 μM, 0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM, 20 μM Incubation Duration: 30 minutes Experimental Results: It shows that KC01 is concentration-dependent Sexual mode inhibits ABHD16A. Lyso-PS measurement in cell culture: Colon cancer cells (COL205, K562, MCF7) or mouse macrophages are treated with KC01 (1 µM) for 4 hours. Cells are harvested, lipids are extracted using Bligh-Dyer or Folch method, and lyso-PS levels are quantified by LC-MS/MS. Cytokine production: Mouse macrophages are treated with KC01 (1 µM) for 4 hours, then stimulated with LPS. Culture supernatants are collected and cytokine levels (e.g., TNF-α, IL-6) are measured by ELISA. |
| Animal Protocol |
Mouse macrophage cytokine production model: Mice are administered KC01 via appropriate route (e.g., intraperitoneal or oral). Peritoneal macrophages or bone marrow-derived macrophages are isolated and stimulated with LPS ex vivo. Cytokine production is measured by ELISA. Alternatively, in vivo LPS challenge model: Mice are treated with KC01 prior to LPS administration, and serum cytokine levels are measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published in the available literature. KC01 has a molecular weight of 365.55 g/mol and molecular formula C₂₂H₃₉NO₃. Comprehensive PK parameters such as bioavailability, half-life, and plasma protein binding remain to be characterized. The compound is a covalent inhibitor.
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| Toxicity/Toxicokinetics |
No toxicity data has been published in the available literature. KC01 is for research use only and has not been fully validated for medical applications. Standard laboratory safety practices should be followed when handling this compound. As an inhibitor of ABHD16A, potential effects on lipid signaling pathways should be considered.
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| References | |
| Additional Infomation |
KC01 is a covalent inhibitor of ABHD16A, a phosphatidylserine lipase that generates lyso-PS. It shows IC50 values of 90 nM for human ABHD16A and 520 nM for mouse ABHD16A. KC01 reduces lyso-PS levels and decreases cytokine production in macrophages. The compound is a valuable tool for studying the role of ABHD16A and lyso-PS in immunomodulation. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C22H39NO3
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|---|---|
| Molecular Weight |
365.56
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| Exact Mass |
365.292
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| Elemental Analysis |
C, 72.28; H, 10.75; N, 3.83; O, 13.13
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| CAS # |
1646795-59-6
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| PubChem CID |
86289046
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
568.7±33.0 °C at 760 mmHg
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| Flash Point |
190.5±21.7 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.514
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| LogP |
5.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
26
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| Complexity |
431
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N)(=O)CCCC/C=C1/C(CCCCCCCCCCCCC)OC/1=O
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| InChi Key |
RJBBAPPWVJEOMC-MNDPQUGUSA-N
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| InChi Code |
InChI=1S/C22H39NO3/c1-2-3-4-5-6-7-8-9-10-11-14-17-20-19(22(25)26-20)16-13-12-15-18-21(23)24/h16,20H,2-15,17-18H2,1H3,(H2,23,24)/b19-16-
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| Chemical Name |
(6Z)-6-(2-oxo-4-tridecyloxetan-3-ylidene)hexanamide
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| Synonyms |
K-C01; K C01; KC01
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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 | 2.7355 mL | 13.6776 mL | 27.3553 mL | |
| 5 mM | 0.5471 mL | 2.7355 mL | 5.4711 mL | |
| 10 mM | 0.2736 mL | 1.3678 mL | 2.7355 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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