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 (98)
Related Products (98)
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Recombinant Proteins (5)
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Antibodies (3)
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CDK5-IN-2
0 ImagesCat. No.: HY-145693CAS No.: 2639542-22-4CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.
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BLINK11
0 ImagesCat. No.: HY-173347BLINK11 is a BBB-penetrant CDK5 inhibitor. BLINK11 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 17.09 nM) and CDK5/p25 (IC50 = 14.69 nM). BLINK11 offers anti-diabetic and neuroprotective benefits. BLINK11 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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CDK7-IN-20
0 ImagesCat. No.: HY-151878CAS No.: 3034210-97-1
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KB-0742 hydrochloride
0 ImagesCat. No.: HY-137478B
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Multi-kinase-IN-7
0 ImagesCat. No.: HY-178142Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum antiproliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.
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BLINK15
0 ImagesCat. No.: HY-173348BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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CDK2-IN-28
0 ImagesCat. No.: HY-161463CAS No.: 3025006-64-5CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM).
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JHK-02-102-1
0 ImagesCat. No.: HY-184913JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications.
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CDK-IN-9
0 ImagesCat. No.: HY-150641CAS No.: 3031561-92-6CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
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Aloisine RP106
0 ImagesAloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively.
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Indirubin-5-sulfonate
0 ImagesCat. No.: HY-111932CAS No.: 244021-67-8Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
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LS-Q2
0 ImagesCat. No.: HY-182986LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
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AG-012986 dihydrochloride
0 ImagesCat. No.: HY-182470CAS No.: 486414-32-8AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity.
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2-Chloroisonicotinamide
0 ImagesCat. No.: HY-115135CAS No.: 100859-84-52-Chloroisonicotinamide is a reagent intermediate. 2-Chloroisonicotinamide can be used for the preparation of CDK5/p25 inhibitors.
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NS-0011
0 ImagesCat. No.: HY-183235CAS No.: 1076234-33-7NS-0011 is a CDK5 inhibitor with a Kd value of 16 μM. NS-0011 binds to the nuclear export signal domain of CDK5, disrupts its interaction with CRM-1 and increases the accumulation of CDK5 in the nucleus. NS-0011 inhibits the proliferation of gastric cancer cells. NS-0011 suppresses the occurrence of gastric cancer xenograft tumors. NS-0011 is applicable to gastric cancer-related research.
