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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V4595 | Simurosertib | 1330782-76-7 | Simurosertib (formerly known as TAK-931) is a novel, selective and orally bioavailable cycle 7(CDC7, cell division cycle 7-related protein)kinase inhibitor with anticancer activity. |
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V1556 | Milciclib (PHA-848125) | 802539-81-7 | Milciclib (formerly also known as PHA-848125; PHA-848125AC; PHA848125) is a novel, potent, ATP-competitive small molecule CDK inhibitor with potential anticancer activity. |
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V1535 | Flavopiridol (Alvocidib) | 146426-40-6 | Flavopiridol (also known as Alvocidib, NSC 649890 HCl;HMR1275;L868275; HMR 1274;NSC649890), a broad spectrum and ATP-competitive inhibitor ofCDKs with potential antineoplastic activity. |
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V1538 | Flavopiridol (Alvocidib) HCl | 131740-09-5 | Flavopiridol HCl(also known as Alvocidib; NSC 649890;HMR-1275; L-868275; HL-275;MDL-107,826A), the HCl salt of flavopiridol which is a flavanoid, is a broad spectrum and ATP-competitive inhibitor ofcyclin-dependent kinases-CDKs with potential antineoplastic activity. |
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V5210 | Olomoucine | 101622-51-9 | Olomoucine,a purine derivative, is a novel and potent CDK (cyclin-dependent kinases) inhibitor that competes for the ATP binding site of the kinase and induces G arrest. |
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V1557 | Palbociclib (PD0332991) Isethionate | 827022-33-3 | Palbociclib Isethionate (formerly known as PD0332991; PD-0332991; Ibrance), the isethionate salt of Palbociclib, is an orally bioavailable pyridopyrimidine-based inhibitor of CDK4/6 with potential antitumor activity and was approved as an anticancer drug. |
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V3044 | Palbociclib (PD-0332991) | 571190-30-2 | Palbociclib (formerly PD-0332991; PD0332991; Pfizer trade nameIbrance) is a highly selective, orally bioavailable pyridopyrimidine-based CDK4/6 inhibitor that has been approved for cancer treatment. |
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V1531 | Palbociclib (PD-0332991) HCl | 827022-32-2 | Palbociclib HCl (Pfizer trade name Ibrance, also known as PD-0332991), the HCl salt of Palbociclib, is a highly selective, orally bioavailable pyridopyrimidine-derived inhibitor of CDK4/6 with potential antineoplastic activity. |
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V0081 | Prexasertib mesylate hydrate (LY 2606368) | 1234015-57-6 | Prexasertib mesylate hydrate (also known as LY2606368 mesylate hydrate) is the hydrated mesylate salt of Prexasertib with potential anticancer activity. |
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V16810 | Trilaciclib (G1T28) | 1374743-00-6 | Trilaciclib (G-1T28; G1T28; Cosela) is a novel, first-in-class and short-acting CDK4/6 inhibitor approved in 2021 by FDA as a medication to reduce the frequency of chemotherapy-induced bone marrow suppression. |
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V31977 | Trilaciclib hydrochloride (G1T28) | 1977495-97-8 | Trilaciclibhydrochloride (G-1T28; Cosela), the hydrochloride salt ofTrilaciclib, is a short-acting CDK4/6 inhibitor with anticancer activity. |
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V5216 | Lerociclib (G1T38) | 1628256-23-4 | Lerociclib (G1T38) is a novel, potent, orally bioavailable and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. |
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V28036 | Voruciclib | 1000023-04-0 | Voruciclib (formerly known as P1446A-05) is a potent and orally bioavailable CDK4/cyclin-dependent kinase 4 inhibitor with potential anticancer activity. |
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V1550 | Ribociclib (LEE011) | 1211441-98-3 | Ribociclib (formerly NVP-LEE011; LEE011; LEE-011; trade name:Kisqali) is a potent, orally bioavailable and highly specific inhibitor of CDK4/6 (cyclin-dependent kinase) with potential antineoplastic activity. |
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V3926 | RIBOCICLIB SUCCINATE HYDRATE | 1374639-79-8 | Ribociclib succinate hydrate (LEE011; LEE-011; NVP-LEE-011; NVP-LEE011; Kisqali), the succinate salt and hydrated form of Ribociclib, is a potent inhibitor of CDK4/6 (cyclin-dependent kinase) (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA for the treatment of breast cancer. |
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V1532 | Seliciclib (Roscovitine) | 186692-46-6 | Seliciclib (also known as Roscovitine, CYC 202; CYC-202;CYC202) is a novel, potent, selective and orally bioavailable small-molecule CDK inhibitor with potential anticancer activity. |
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V0079 | Prexasertib mesylate (LY-2606368 mesylate) | 1234015-55-4 | Prexasertib mesylate (also known as LY2606368 mesylate) is a novel, potent, selective and ATP competitive inhibitor of the CHK1 (checkpoint kinase 1) protein kinase with potential anticancer activity. |
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V0080 | Prexasertib 2HCl (LY-2606368) | 1234015-54-3 | Prexasertib 2HCl (also known as LY2606368) is the dihydrochloride salt of Prexasertib with potential anticancer activity. |
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V3924 | Ribociclib HYDROCHLORIDE | 1211443-80-9 | Ribociclib HCl (formerly also known as LEE-011; NVP-LEE011; Kisqali), the hydrochloride salt ofRibociclib, is an orally bioavailable CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA to treat postmenopausal women with a type of advanced breast cancer. |
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V1551 | Manidipine 2HCl | 89226-75-5 | Manidipine 2HCl (alsocalled CV-4093;CV4093), the dihydrochloride saltform of Manidipine, is a calcium channel blocker/CCB that is used clinically as an antihypertensive agent. |
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