| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 250mg | |||
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| Targets |
CKI-7 free base targets casein kinase 1 (CK1) as an ATP-competitive inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. It also selectively inhibits Cdc7 kinase, SGK, ribosomal S6 kinase-1 (S6K1), and mitogen- and stress-activated protein kinase-1 (MSK1). It is much less potent against CK2 and other protein kinases.
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| ln Vitro |
In ES cells, CKI-7 treatment (0.1-10 μM; 5 days) dramatically enhanced the number of cells positive for the neural markers βIII-tubulin and nestin, as well as the expression of the early neuroectoderm marker Sox1 in a concentration-dependent manner [1]. Day 5 β-catenin stabilization induced by SFEB was decreased by CKI-7 (5 μM; 5 days; ES cells) treatment, suggesting that CKI-7 suppresses Wnt signaling [1].
In vitro, CKI-7 free base potently inhibits CK1 with an IC50 of 6 μM and a Ki of 8.5 μM. It selectively inhibits Cdc7 kinase and also inhibits SGK, S6K1, and MSK1. It is much less potent against casein kinase II and other protein kinases. The compound is used as a research tool to study CK1-mediated signaling pathways. |
| ln Vivo |
Using a newly isolated Philadelphia chromosome-positive acute lymphoblastic leukemia cell line, the in vivo dose-dependent anticancer efficacy of CKI-7 was established in a SCID-Beige mouse systemic tumor model. The activation of caspase 3 and subsequent cell cycle-dependent death are confirmed by standard cell cycle synchronization tests upon exposure to CKI-7 [2].
In vivo, CKI-7 free base is used as a research tool to study the role of CK1 and other kinases in various biological processes. As a kinase inhibitor, it can be administered to animal models to study the effects of CK1 inhibition on cell cycle regulation, Wnt signaling, and other pathways. Detailed in vivo pharmacokinetic and efficacy studies are limited. |
| Enzyme Assay |
CKI-7 free base is evaluated in vitro for its inhibitory activity against CK1 and other kinases. Kinase assays are performed using recombinant enzymes and peptide substrates with ³³P-ATP or luminescence-based detection. The compound is incubated with increasing concentrations, and IC50 values are calculated. Selectivity is confirmed by testing against a panel of kinases including CK2, Cdc7, SGK, S6K1, and MSK1.
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| Cell Assay |
RT-PCR[1]
Cell Types: Mouse ES cells Tested Concentrations: 0.1-10 μM Incubation Duration: 5 days Experimental Results: The expression of early neuroectoderm marker Sox1 was Dramatically increased, and the neural markers nestin and βIII-tubulin were Dramatically increased. The number of positive cells increased Dramatically in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: Mouse ES cells Tested Concentrations: 5 μM Incubation Duration: 5 days Experimental Results: Inhibition of SFEB-induced β-catenin stabilization on day 5. For in vitro cell-based assays, cells are cultured and treated with CKI-7 free base at various concentrations. CK1 inhibition is confirmed by measuring the phosphorylation of CK1 substrates via Western blot. Cell cycle analysis is performed by propidium iodide staining and flow cytometry. The compound's effects on Wnt signaling and other CK1-regulated pathways are assessed. Cell viability is measured by MTT or standard assays. |
| Animal Protocol |
In vivo animal studies with CKI-7 free base are limited. The compound could be administered to rodent models to study the role of CK1 in various diseases. However, specific published protocols are limited. The compound is primarily used as a research reagent for in vitro studies of CK1 and related kinases.
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| ADME/Pharmacokinetics |
CKI-7 free base (CAS: 120615-25-0) has a molecular weight of 285.75 g/mol and a molecular formula of C11H12ClN3O2S. It is also known as N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide. Solubility: DMSO 25 mg/mL. Storage: powder at -20°C for 3 years; in solvent at -80°C for 6 months. Purity: >99%.
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| Toxicity/Toxicokinetics |
CKI-7 free base is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile at research concentrations. As a kinase inhibitor, it may have effects on normal cell cycle progression and signaling pathways. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide belongs to the isoquinoline class of compounds. Its structure is isoquinoline-8-sulfonamide with a chlorine-substituted 5-position, where the nitrogen atom of the sulfonamide is replaced by a 2-aminoethyl group. It is an inhibitor of casein kinase I, belonging to EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitors. It is a sulfonamide compound, belonging to the isoquinoline class, an organochlorine compound, and also a primary amino compound.
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. It selectively inhibits Cdc7 kinase and also inhibits SGK, S6K1, and MSK1. It is much less potent against casein kinase II and other protein kinases. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C₁₁H₁₂CLN₃O₂S
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|---|---|
| Molecular Weight |
285.75
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| Exact Mass |
285.034
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| CAS # |
120615-25-0
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| Related CAS # |
CKI-7;1177141-67-1
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| PubChem CID |
129236
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.432g/cm3
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| Boiling Point |
499.7ºC at 760mmHg
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| Melting Point |
188-190ºC
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| Flash Point |
256ºC
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| Vapour Pressure |
4.04E-10mmHg at 25°C
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| Index of Refraction |
1.644
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| LogP |
3.297
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OGKYMFFYOWUTKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12ClN3O2S/c12-10-1-2-11(18(16,17)15-6-4-13)9-7-14-5-3-8(9)10/h1-3,5,7,15H,4,6,13H2
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| Chemical Name |
N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide
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| Synonyms |
CKI7 free base; CKI 7 free base
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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) |
DMSO : ~25 mg/mL (~87.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4996 mL | 17.4978 mL | 34.9956 mL | |
| 5 mM | 0.6999 mL | 3.4996 mL | 6.9991 mL | |
| 10 mM | 0.3500 mL | 1.7498 mL | 3.4996 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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