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Purity: ≥98%
CK-636 (also called CK636; CK-0944636; CK0944636) is a potent inhibitor of the actin-related protein (Arp2/3) complex with IC50 values of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively. CK-636 binds between Arp2 and Arp3 where it appears to block movement of Arp2 and Arp3 into their active conformation and inhibits Arp2/3 complex’s ability to nucleate actin filaments. In a concentration dependence way, CK-636 reduced the formation of actin filament comet tails by Listeria with IC50 value of 22 μM in infected SKOV3 cells.
| ln Vitro |
Arp2 and Arp3 appear to be prevented from adopting their active conformations by CK-636, which binds between them. CK-636 modifies the conformation of Arp3 by inserting into its hydrophobic core. Infected SKOV3 cells (IC50=22 μM), CK-636 inhibits actin polymerization and Listeria monocytogenes' production of actin filament comet tails [1]. T cells treated with CK-636 also exhibited an elongated morphology with sharp pseudopodia at the leading edge, and their width was roughly 30% less than that of T cells treated with DMSO [2].
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| ln Vivo |
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| References |
[1]. Nolen BJ, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4.
[2]. Kwon KW, et al. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960. [3]. Liang Ma, et al. Discovery of the migrasome, an organelle mediating release of cytoplasmic contents during cell migration. Cell Res. 2015 Jan;25(1):24-38. |
| Molecular Formula |
C16H16N2OS
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| Molecular Weight |
284.38
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| CAS # |
442632-72-6
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| Related CAS # |
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| SMILES |
S1C([H])=C([H])C([H])=C1C(N([H])C([H])([H])C([H])([H])C1=C(C([H])([H])[H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O
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| InChi Key |
ACAKNPKRLPMONU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16N2OS/c1-11-12(13-5-2-3-6-14(13)18-11)8-9-17-16(19)15-7-4-10-20-15/h2-7,10,18H,8-9H2,1H3,(H,17,19)
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| Chemical Name |
N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5164 mL | 17.5821 mL | 35.1642 mL | |
| 5 mM | 0.7033 mL | 3.5164 mL | 7.0328 mL | |
| 10 mM | 0.3516 mL | 1.7582 mL | 3.5164 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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