CDK
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<div class="colum_1 clearer"><p>CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.</p><p>There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.</p><p>CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of <i>S. pombe</i> (Cdc2), <i>S. cerevisia</i> (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).</p></div>
Products Related to CDK(299)
- GC68845CDK12-IN-5CAS: 2651200-35-8Purity: >98%
CDK12-IN-5 is a pyrazole-triazine compound that is an effective inhibitor of CDK12, with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).
- GC68847CDK2-IN-13CAS: 101622-53-1Purity: >98.00%
CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 value of 12 μM. CDK2-IN-13 can be used for cancer research.
- GC68848CDK4/6-IN-15CAS: 2078047-99-9Purity: >98%
CDK4/6-IN-15 is an orally effective and selective CDK4/6 inhibitor. It can effectively inhibit cancer cell growth. CDK4/6-IN-15 blocks the cell cycle in the G1 phase and inhibits phosphorylation of retinoblastoma tumor suppressor protein (Rb) at S780 site and E2 factor (E2F)-regulated gene expression in retinoblastoma tumors.
- GC68979DIF-3CAS: 113411-17-9Purity: >98.00%
DIF-3 promotes the degradation of GSK-3β and reduces the expression levels of cyclin D1 and c-Myc. It inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 has a strong anti-proliferative effect on human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression.
- GC69747PROTAC CDK12/13 Degrader-1Purity: >98%
PROTAC CDK12/13 Degrader-1 (7f) is a highly efficient and selective dual degrader of cell cycle-dependent kinases CDK12/CDK13, with DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used for breast cancer research.
- GC69987TanuxiciclibCAS: 1983983-64-7Purity: >98%
Tanuxiciclib is a cell cycle cyclin-dependent kinase (CDK) inhibitor.
- GC69988Tanuxiciclib trihydrochlorideCAS: 1983984-11-7Purity: >98.00%
Tanuxiciclib trihydrochloride is a cell cycle cyclin-dependent kinase (CDK) inhibitor.
- GC71063Akt1&PKA-IN-1CAS: 1334107-58-2
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively.
- GC72931HTH-01-091 TFAPurity: >98.00%
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM.
- GC72951CDK9 inhibitor HH1CAS: 204188-41-0Purity: >99.50%
CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor.
- GC73053BSJ-03-204 triTFAPurity: >99.00%
BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK.
- GC73063Tagtociclib hydrateCAS: 2733575-91-0Purity: >99.00%
PF-07104091 drate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively.
- GC73086CDK4/6-IN-15 hydrochloridePurity: >99.00%
CDK4/6-IN-15 drochloride is an orally active and selective CDK4/6 inhibitor.
- GC73183CDK8-IN-12CAS: 2613307-67-6Purity: >99.00%
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC67970 | DD-03-156 | - | >98% | |
| GC68455 | CP681301 | 865317-32-4 | >98% | |
| GC68712 | AZ5576 | 2751721-40-9 | >99.00% | |
AZ5576 is a potent and highly selective inhibitor of CDK9 (IC50: | ||||
| GC68845 | CDK12-IN-5 | 2651200-35-8 | >98% | |
CDK12-IN-5 is a pyrazole-triazine compound that is an effective inhibitor of CDK12, with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1). | ||||
| GC68846 | CDK1-IN-2 | 220749-41-7 | >97.00% | |
CDK1-IN-2 is a CDK1 inhibitor (IC50: 5.8 μM). | ||||
| GC68847 | CDK2-IN-13 | 101622-53-1 | >98.00% | |
CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 value of 12 μM. CDK2-IN-13 can be used for cancer research. | ||||
| GC68848 | CDK4/6-IN-15 | 2078047-99-9 | >98% | |
CDK4/6-IN-15 is an orally effective and selective CDK4/6 inhibitor. It can effectively inhibit cancer cell growth. CDK4/6-IN-15 blocks the cell cycle in the G1 phase and inhibits phosphorylation of retinoblastoma tumor suppressor protein (Rb) at S780 site and E2 factor (E2F)-regulated gene expression in retinoblastoma tumors. | ||||
| GC68885 | CLK1-IN-2 | - | >98.00% | |
CLK1-IN-2 is a metabolically stable inhibitor of Clk1. It has selective activity against Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for research on tumors, Duchenne muscular dystrophy, and viral infections such as HIV-1 and influenza. | ||||
| GC68898 | CPS2 | 2756741-90-7 | >98% | |
CPS2 is a highly efficient, selective, and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for research on acute myeloid leukemia. | ||||
| GC68979 | DIF-3 | 113411-17-9 | >98.00% | |
DIF-3 promotes the degradation of GSK-3β and reduces the expression levels of cyclin D1 and c-Myc. It inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 has a strong anti-proliferative effect on human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression. | ||||
| GC69747 | PROTAC CDK12/13 Degrader-1 | - | >98% | |
PROTAC CDK12/13 Degrader-1 (7f) is a highly efficient and selective dual degrader of cell cycle-dependent kinases CDK12/CDK13, with DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used for breast cancer research. | ||||
| GC69987 | Tanuxiciclib | 1983983-64-7 | >98% | |
Tanuxiciclib is a cell cycle cyclin-dependent kinase (CDK) inhibitor. | ||||
| GC69988 | Tanuxiciclib trihydrochloride | 1983984-11-7 | >98.00% | |
Tanuxiciclib trihydrochloride is a cell cycle cyclin-dependent kinase (CDK) inhibitor. | ||||
| GC71063 | Akt1&PKA-IN-1 | 1334107-58-2 | - | |
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. | ||||
| GC72931 | HTH-01-091 TFA | - | >98.00% | |
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. | ||||
| GC72951 | CDK9 inhibitor HH1 | 204188-41-0 | >99.50% | |
CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. | ||||
| GC73007 | DB18 | 2587177-94-2 | >98.00% | |
DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC50 values in the range of 10-30 nM for CLK1, CLK2 and CLK4. | ||||
| GC73053 | BSJ-03-204 triTFA | - | >99.00% | |
BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. | ||||
| GC73063 | Tagtociclib hydrate | 2733575-91-0 | >99.00% | |
PF-07104091 drate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. | ||||
| GC73086 | CDK4/6-IN-15 hydrochloride | - | >99.00% | |
CDK4/6-IN-15 drochloride is an orally active and selective CDK4/6 inhibitor. | ||||
| GC73100 | Senexin C | 2375554-02-0 | >98.00% | |
Senexin C is a selective and orally active CDK8/19 inhibitor. | ||||
| GC73183 | CDK8-IN-12 | 2613307-67-6 | >99.00% | |
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. | ||||
| GC73219 | LL-K8-22 | - | >99.00% | |
LL-K8-22 is a potent, selective and durable CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. | ||||
| GC73224 | CLK1-IN-3 | 2922550-28-3 | >98.00% | |
CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. | ||||
