CDK5
CDK5 is a proline-directed serine/threonine kinase that controls neuronal development, postsynaptic signal integration, neurotransmitter release, and neurite outgrowth[1][2]. Mechanistically, CDK5 activity depends on neural activators such as p35, and p35-deficient mice show cortical lamination defects, seizures, and adult lethality[3][4]. In disease models, calpain-mediated conversion of p35 to p25 deregulates CDK5 activity and promotes neurodegeneration, linking the CDK5-p25 axis to tau phosphorylation research[5]. Compared with proliferative CDKs, CDK5 differs because p35 or p39 binding activates it, whereas Tyr-15 phosphorylation does not activate the CDK5-p35 complex[6]. For experimental applications, roscovitine inhibits cdc2, CDK2, and CDK5, while p35-derived peptides specifically inhibit deregulated CDK5 activity[7][8].
References:
- [1]. Kim SH, et al. CDK5 serves as a major control point in neurotransmitter release. Neuron. 2010 Sep 9;67(5):797-809. [Content Brief]
- [2]. Nikolic M, et al. The cdk5/p35 kinase is essential for neurite outgrowth during neuronal differentiation. Genes Dev. 1996 Apr 1;10(7):816-25. [Content Brief]
- [3]. Tsai LH, et al. p35 is a neural-specific regulatory subunit of cyclin-dependent kinase 5. Nature. 1994 Sep 29;371(6496):419-23. [Content Brief]
- [4]. Chae T, et al. Mice lacking p35, a neuronal specific activator of Cdk5, display cortical lamination defects, seizures, and adult lethality. Neuron. 1997 Jan;18(1):29-42. [Content Brief]
- [5]. Patrick GN, et al. Conversion of p35 to p25 deregulates Cdk5 activity and promotes neurodegeneration. Nature. 1999 Dec 9;402(6762):615-22. [Content Brief]
- [6]. Kobayashi H, et al. Phosphorylation of cyclin-dependent kinase 5 (Cdk5) at Tyr-15 is inhibited by Cdk5 activators and does not contribute to the activation of Cdk5. J Biol Chem. 2014 Jul 11;289(28):19627-36. [Content Brief]
- [7]. Meijer L, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36. [Content Brief]
- [8]. Kesavapany S, et al. Peptides derived from Cdk5 activator p35, specifically inhibit deregulated activity of Cdk5. Biotechnol J. 2007 Aug;2(8):978-87. [Content Brief]
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CDK5 Related Products (97)
Related Products (97)
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Recombinant Proteins (5)
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Antibodies (3)
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CGP60474
0 ImagesCGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
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PHA-767491 hydrochloride
0 ImagesSynonyms: CAY-10572 hydrochloridePHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
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MeBIO
0 ImagesMeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.
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(R)-CR8 trihydrochloride
0 ImagesSynonyms: CR8, (R)-Isomer trihydrochloride(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
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PHA-767491
0 ImagesSynonyms: CAY10572PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
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Samuraciclib
0 ImagesSynonyms: CT7001; ICEC0942Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects.
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CDK5 inhibitor 20-223
0 ImagesSynonyms: CP668863CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
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Purvalanol B
0 ImagesCat. No.: HY-18299CAS No.: 212844-54-7Synonyms: NG 95Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
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Lerociclib dihydrochloride
0 ImagesSynonyms: G1T38 dihydrochloride
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GW8510
0 ImagesGW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities.
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Lerociclib
0 ImagesSynonyms: G1T38Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
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CDK5-IN-3
0 ImagesCDK5-IN-3 (compound 11) is a potent CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).
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Samuraciclib hydrochloride dihydrate
0 ImagesCat. No.: HY-103712BPurity: 99.90%Synonyms: CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrateSamuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.
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TMX-3013
0 ImagesTMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).
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Olomoucine
0 ImagesOlomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.
