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| SKU | Size | Availability |
Price | Qty |
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C650922-5mg
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5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$450.90
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C650922-10mg
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10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$750.90
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C650922-25mg
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25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$1,500.90
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| Specifications & Purity | ≥99% |
|---|---|
| Biochemical and Physiological Mechanisms | CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM. |
| Storage Temp | Store at -20°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM. In Vitro CLK1 is the most potently inhibited kinase (IC 50 : 2 nM). In addition to CLK1, only two kinases have an IC 50 value less than 100 nM, namely CLK2 (IC 50 : 31 nM) and CLK4 (IC 50 : 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CLK1 2 nM (IC 50 ) |
Taxonomy Tree
| Kingdom | Organic compounds |
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| Superclass | Organoheterocyclic compounds |
| Class | Azoles |
| Subclass | Triazoles |
| Intermediate Tree Nodes | Phenyltriazoles |
| Direct Parent | Phenyl-1,2,3-triazoles |
| Alternative Parents | Quinolines and derivatives Benzoxazoles Fluorobenzenes Pyridines and derivatives Aryl fluorides Oxazoles Heteroaromatic compounds Oxacyclic compounds Azacyclic compounds Organopnictogen compounds Organooxygen compounds Organonitrogen compounds Organofluorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Phenyl-1,2,3-triazole - Quinoline - Benzoxazole - Halobenzene - Fluorobenzene - Benzenoid - Pyridine - Monocyclic benzene moiety - Aryl halide - Aryl fluoride - Heteroaromatic compound - Oxazole - Oxacycle - Azacycle - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as phenyl-1,2,3-triazoles. These are organic compounds containing a 1,2,3-triazole substituted by a phenyl group. |
| External Descriptors | Not available |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| IUPAC Name | 5-[1-[(1S)-1-(4-fluorophenyl)ethyl]triazolo[4,5-c]quinolin-8-yl]-1,3-benzoxazole |
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| INCHI | InChI=1S/C24H16FN5O/c1-14(15-2-6-18(25)7-3-15)30-24-19-10-16(4-8-20(19)26-12-22(24)28-29-30)17-5-9-23-21(11-17)27-13-31-23/h2-14H,1H3/t14-/m0/s1 |
| InChIKey | BHKVSOQUPYXVRZ-AWEZNQCLSA-N |
| Smiles | CC(C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6 |
| Isomeric SMILES | C[C@@H](C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6 |
| PubChem CID | 129318964 |
| Molecular Weight | 409.42 |
| Solubility | DMSO : 25 mg/mL (61.06 mM; Need ultrasonic) |
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