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Roscovitine Roscovitine is a potent and selective inhibitor of cyclin-dependent kinases (CDKs). Roscovitine has been found to produce apoptosis in treated cancerous cells of non-small cell lung cancer (NSCLC) and other cancers. Studies show that Roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle. Roscovitine maybe useful in the treatment of non-small cell lung cancer (NSCLC), leukemia, HIV infection, herpes simplex infection, and the mechanisms of chronic inflammation disorders. Group: Biochemicals. Alternative Names: (2R)-2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; (R)-2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine; CYC 202; (R)-Roscovitine; R-Roscovitine; Roscovitin; Seliciclib. Grades: Highly Purified. CAS No. 186692-46-6. Pack Sizes: 25mg. US Biological Life Sciences. USBiological 2
Worldwide
Aftin-4 (N6-Methyl-(R)-roscovitine, Amyloid-beta Forty-Two Inducer 4) Roscovitine-related purine with no activity on CDKs (used as control for roscovitine). Selectively and potently increases production of extracellular Abeta42 and decreases production of extracellular Abeta38 in cultured cells. Extracellular Abeta40 levels remain stable. Intracellular levels of these amyloids appear to remain stable. Alzheimer's Disease (AD) accelerator that interacts with VDAC1, prohibitin and mitofilin, possibly interfering with subcellular compartmentalization and lipid rafts properties, shifting gamma-secretase activity toward Abeta42 generation. Induces a reversible mitochondrial phenotype reminiscent of the one observed in AD brains. Tool to detect inhibitors of Aftin-induced actions (potential anti-AD compounds). Binds pyridoxal kinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 866893-90-5. Pack Sizes: 1mg, 5mg, 25mg. US Biological Life Sciences. USBiological 4
Worldwide
(R)-Roscovitine Potent and selective inhibitor of CDKs. More potent than olomoucine. Inhibits CDK1/cyclin B kinase (IC50 = 450nM), CDK2 (IC50 = 700nM) and CDK5/p35 (IC50 = 160nM). Inhibits M phase promoting factor (MPF) kinase activity. Arrests human fibroblasts in G1 phase. Antitumor compound. Activates the mitogen-activated protein kinase pathway. Targets both the p53 and NF-kappaB pathways. Has effects on calcium channel gating. Prevents DNA damage-induced cyclin A1 upregulation. Apoptosis inducer. As CYC202 in phase I clinical trials. Group: Biochemicals. Alternative Names: (2R)-2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; (R)-2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine; CYC 202; (R)-Roscovitine; R-Roscovitine; Roscovitin; Seliciclib. Grades: Highly Purified. CAS No. 186692-46-6. Pack Sizes: 1mg, 5mg, 50mg. Molecular Formula: C??H??N?O. US Biological Life Sciences. USBiological 3
Worldwide
(R)-Roscovitine (R)-Roscovitine (Seliciclib) is an orally bioavailable and selective CDKs inhibitor with IC 50 s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5 , Cdc2 , and CDK2 , respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Seliciclib; CYC202. CAS No. 186692-46-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-30237. MedChemExpress MCE
6-Amino-1-hexanol 6-Amino-1-hexanol is used in the synthesis of guanidino analogs of roscovitine, which is a cyclin-dependant kinase. Also used in the preparation of tocotrienols which maintain anticancer, antiproliferative and antimigratory activity. Group: Biochemicals. Grades: Highly Purified. CAS No. 4048-33-3. Pack Sizes: 10g, 25g, 100g. Molecular Formula: C?H??NO. US Biological Life Sciences. USBiological 3
Worldwide
6-Amino-1-hexanol A reagent used in the synthesis of guanidino analogs of roscovitine. Synonyms: H-Acp(6)-ol; NH2-(CH2)6-OH; ζ-Amino-n-hexyl alcohol; 6-Amino-N-caproyl alcohol. Grades: ≥ 99 % (GC). CAS No. 4048-33-3. Molecular formula: C6H15NO. Mole weight: 117.19. BOC Sciences 4
Aftin-5 ((2R)-2-[[9-Isopropyl-6-(N-methylanilino)purin-2-yl]amino]butan-1-ol, Amyloidbeta Forty-Two Inducer 5) Roscovitine-related purine with no activity on CDKs (used as control for roscovitine). Selectively and potently increases production of extracellular Ab42 and decreases production of extracellular Ab38 in cultured cells. Extracellular Ab40 levels remain stable. Intracellular levels of these amyloids appear to remain stable. Alzheimer's Disease (AD) accelerator that interacts with VDAC1, prohibitin and mitofilin, possibly interfering with subcellular compartmentalization and lipid rafts properties, shifting gamma-secretase activity toward Ab42 generation. Induces a reversible mitochondrial phenotype reminiscent of the one observed in AD brains. Tool to detect inhibitors of Aftin-induced actions (potential anti-AD compounds). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 5mg, 25mg. US Biological Life Sciences. USBiological 4
Worldwide
Bohemine Bohemine, structurally similar to Olomoucine and Roscovitine, is a 2,6,9-trisubstituted purine derivative that inhibits cyclin-dependent kinases (CDKs) and exhibits anticancer activity. Synonyms: 3-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]propan-1-ol; 6-benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine; bohemine. Grades: ≥97%. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42. BOC Sciences 10
CR8 CR8 is a potent and selective inhibitor of CDK. CR8 is a more potent pyridyl analogue of roscovitine. In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. (R)?-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K. Synonyms: (R)-CR8; CR 8; CR-8. Grades: 98%. CAS No. 294646-77-8. Molecular formula: C24H29N7O. Mole weight: 431.544. BOC Sciences 11
Ibulocydine Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibulocydine rapidly blocked phosphorylation of the carboxyl-terminal domain (CTD) of the large subunit of RNA polymerase II, a process mediated by Cdk7/9. Anti-apoptotic gene products such as Mcl-1, survivin, and X-linked IAP (XIAP) are crucial for the survival of many cell types, including HCC. Following the inhibition of RNA polymerase II phosphorylation, ibulocydine caused rapid down-regulation of Mcl-1, survivin, and XIAP, thus inducing apoptosis. Furthermore, ibulocydine effectively induced apoptosis in HCC xenografts with no toxic side effects. These results suggest that ibulocydine is a strong candidate anti-cancer drug for the treatment of HCC. Synonyms: Ibulocydine. Grades: 98%. CAS No. 1314096-68-8. Molecular formula: C16H20BrN5O6. Mole weight: 458.26. BOC Sciences 11
Seliciclib Seliciclib is an orally bioavailable, small-molecule cyclin-dependent kinase (CDK) inhibitor with potential proapoptotic and antineoplastic activities. Seliciclib primarily inhibits CDK2/E, CDK2/A, CDK7 and CDK9 by competing for their ATP binding sites, leading to a disruption of cell cycle progression. In addition, this agent appears to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, inhibiting RNA polymerase II-dependent transcription, which may result in the down-regulation of antiapoptotic proteins such as induced myeloid leukemia cell differentiation protein Mcl-1. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Mcl-1 belongs to the Bcl-2 family of antiapoptotic proteins and is a protein crucial to the survival of a range of tumor cell types. Synonyms: R-roscovitine. CYC202; CYC202; CYC 202; R-Roscovitine; Roscovitin; Roscovitine; Seliciclib. R-Roscovitine; Roscovitin; Roscovitine. Grades: >98%. CAS No. 186692-46-6. Molecular formula: C19H26N6O. Mole weight: 354.44. BOC Sciences 10

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