CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle.Additionally, they control mRNA processing, transcription, and nerve cell differentiation. With molecular weights between 34 and 40 kDa, CDKs are relatively small proteins that only contain the kinase domain. In fact, when their CDK gene has been replaced with the homologous human gene, yeast cells can proliferate normally. A CDK by definition binds the control protein cyclin. Only the cyclin-CDK complex is an active kinase; CDK lacks much kinase activity on its own.
Around 20 Cyclin-dependent kinases (CDK1-20) have been identified as of yet. While CDK 7, 8, 9 and 11 are linked to transcription, CDK1, 4, and 5 are involved in the cell cycle.
The majority of CDK regulation occurs post-translationally, and CDK levels are essentially constant throughout the cell cycle. The majority of knowledge about CDK structure and function is based on CDKs from vertebrates (CDC2 and CDK2), S. pombe (CDC28), and S. cerevisiae (Cdc2). Cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and CDK inhibitory subunit (CKI) binding are the four main mechanisms of CDK regulation.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V77305 | Abemaciclib metabolite M2-d6 (LSN2839567-d6) | Abemaciclib metabolite M2-d6 is the deuterium labelled form of Abemaciclib metabolite M2. | |
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V77306 | Abemaciclib metabolite M20-d8 (LSN3106726-d8) | Abemaciclib metabolite M20-d8 is the deuterium labelled form of Abemaciclib metabolite M20. | |
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V52536 | Abemaciclib-d8 (LY2835219-d8) | 2088650-53-5 | Abemaciclib-d8 is the deuterium labelled form of Abemaciclib. |
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V55069 | Akt1&PKA-IN-1 | 1334107-58-2 | Akt1&PKA-IN-1 is a potent Akt/PKA dual (bifunctional) inhibitor (antagonist) with IC50s of 0.03, 0.11 μM and 9.8 μM for PKAa, Akt and CDK2, respectively. |
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V55068 | Akt1&PKA-IN-2 | 1334108-00-7 | Akt1&PKA-IN-2 ((R)-29) is a cyclin-dependent kinase 2 (CDK2)-selective amide PKB/AKT inhibitor. |
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V5083 | Alsterpaullone | 237430-03-4 | Alsterpaullone (also known as 9-Nitropaullone and NSC-705701; NSC 705701) is a novel and potent ATP-competitive cyclin-dependent kinases (CDK) inhibitor with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. |
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V75985 | Anticancer agent 29 | 2907774-89-2 | Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent with IC50s of 0.054 μM, 0.127 μM, 0.129 μM, and 0.396 μM for CDK2, CDK1, CDK4, and CDK6, respectively. |
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V75987 | Anticancer agent 30 | 2907774-88-1 | anti-cancer compound 30 (compound 6f-Z) is a 3-arylidene-2-oxindole analogue, a selective CDK2 inhibitor (antagonist) with potent anti-cancer effect. |
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V55085 | Antitumor agent-104 | 2245272-16-4 | Antitumor agent-104 (Compound 9) is an antitumor agent that works by inhibiting the repair of DNA damage in tumors. |
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V2745 | ARS-853 | 1629268-00-3 | ARS-853 is a novel, potent, selective, and covalent inhibitor of KRAS(G12C) with IC50 of 2.5 μM. |
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V52393 | AS2863619 | 2241300-51-4 | AS2863619 can convert antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells to study various immune diseases. |
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V11793 | AT-7519 diHCl | 902135-91-5 | AT-7519 diHCl is a novel and potent multi-CDK (cyclin-dependent kinase) inhibitor for Cdk1/cyclin B, Cdk2/Cyclin A, Cdk3/Cyclin E, Cdk4/Cyclin D1, Cdk5/p35, and Cdk6/Cyclin D3 with IC50s of 210, 47, 100, 13, 170, and<10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. |
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V1537 | AT7519 | 844442-38-2 | AT7519 (AT-7519; AT 7519) is an orally bioavailable and potent inhibitor of multiple CDKs (cyclin-dependent kinases) with potential antitumor activity. |
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V1539 | AT7519 HCl | 902135-91-5 | AT7519 HCl, the hydrochloride salt of AT7519 (AT-7519), is a potent, orally bioavailable small molecule CDK inhibitor with potential anticancer activity. |
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V32873 | AT7519 trifluoroacetate | 1431697-85-6 | AT7519 trifluoroacetate is an orally bioavailable small molecule, potent andmulti-CDK (cyclin-dependent kinase) inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. |
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V3687 | Atuveciclib (BAY-1143572) | 1414943-88-6 | Atuveciclib (formerly known as BAY-1143572) is novel, potent, oral and highly selective PTEFb/CDK9 inhibitor with antitumor activity. |
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V7882 | Atuveciclib (BAY-1143572) | 2923012-24-0 | Atuveciclib (BAY-1143572) is a potent, orally bioactive and selective PTEFb/CDK9 inhibitor. |
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V3689 | Atuveciclib racemate | 1414943-88-6 | Atuveciclib racemate (formerly BAY-1143572 racemate) is the racemic mixture of Atuveciclib, which is novel, potent, oral and highly selective PTEFb/CDK9 inhibitor currently in Phase I clinical trial to treat cancer. |
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V3688 | Atuveciclib S-Enantiomer | Atuveciclib S-enantiomer (formerly known as BAY-1143572), the S-isomer of Atuveciclib, is novel, potent, orally bioactive and highly selective PTEFb/CDK9 inhibitor. | |
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V75976 | Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) | 2250279-81-1 | Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and specific CDK9 inhibitor that can suppress CDK9/CycT1 with IC50 of 16 nM. |
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