CAT # | Product Name | Descriptio |
CPD100904 | Voruciclib | Voruciclib, etiam ut P1446A-05, est interdum inhibitor kinasus specificae pro cyclino-dependens kinase 4 (CDK4) cum actu antineoplastico potentiale. CDK4 inhibitor P1446A-05 specialiter vetat CDK4 mediatum G1-S tempus transitus, cellam cyclicam capiens et incrementum cellae cancer inhibens. Serinum/threoninum kinasum CDK4 in complexu cum D-type G1 cyclinis invenitur et primum kinasus ad excitationem mitogenicam reducitur, cellulas a quiescente stadio in G1/S activitate cycli solvens; Complexiones CDK-cyclinae ostensae sunt phosphorylate retinoblastomae (Rb) transcriptionis factoris in primo G1, ac divellens histonum deacetylasium (HDAC) et reprimendum transcriptionale interclusio. |
CPD100905 | Alvocidib | Alvocidib synthetica N-methylpiperidinyl chlorophenyl flavone compositum est. Sicut inhibitor cyclini-dependens kinasis, alvocidib cycli cellulae comprehensionem inducit impediendo phosphorylationem cyclini-dependens kinases (CDKs) et cyclinum D1 et D3 descensum expressio, inde in G1 cycli cellulae comprehensio et apoptosis. Hoc agens est etiam competitive inhibitor actionis adenosinae triphosphatae. Compesce pro iudiciis clinicis activis vel iudiciis clinicis clausis hoc agente utens. |
CPD100906 | BS-181 | BS-181 valde selectivum CDK inhibitor pro CDK7 cum IC(50) 21 nmol/L. Probatio aliarum CDKs ac aliorum 69 kinases ostendebant BS-181 solum CDK2 inhiberi in concentratione minore quam 1 micromol/L, cum CDK2 inhibitis 35-ovilibus minus potenter (IC(50) 880 nmol/L) quam CDK7. In cellulis MCF-7, BS-181 phosphorylationem CDK7 subiectarum inhibuit, cycli cycli promovendi comprehensionem et apoptosim ad inhibenda linearum cellularum cancri incrementum inhibuit et effectus in vivo antitumorem ostendit. |
CPD100907 | Riviciclib | Riviciclib, etiam P276-00 cognominatus, est flavonus et cyclinus kinasus dependens (CDK) inhibitor cum actione antineoplastica potentiale. P276-00 selective adstringit et vetat Cdk4/cyclinum D1, Cdk1/cyclinum B et Cdk9/cyclinum T1, serina/threonina kinases quae in moderandis cycli cellulis et multiplicatione cellularum functiones agunt. Inhibitio harum kinasium ducit ad comprehensionem cycli cellularum per transitum G1/S, inde inductionem apoptosis et inhibitionem tumoris cellulae multiplicationis. |
CPD100908 | MC180295 | MC180295 inhibitor selectivorum CDK9 (IC50 = 5 nM). (MC180295 lata est anti-cancri actio in vitro et efficax in exemplaribus cancri vivorum. Accedit CDK9 inhibitio sensum immunem LAPIS inhibitoris α-PD-1 in vivo, quod egregium scopum epigeneticae therapiae cancri facit. |
1073485-20-7 | LDC000067 | LDC000067 potens est CDK9 inhibitor et selectivus. LDC000067 in vitro transcriptionis inhibetur modo ATP-competitivo et dosis dependens. Gene expressio profiling cellularum cum LDC000067 tractatarum demonstravit selectivam reductionem brevium variantium, inter regulatores magni momenti proliferation et apoptosin. Analysis de novo RNA synthesis suggessit amplum munus positivum CDK9. In gradu hypothetico et celluloso, LDC000067 reproducti effectus propriae inhibitionis CDK9 quales sunt RNA polymerase II in genes intermissa, ac potissimum inductio apoptosis in cellulis cancri. LDC000067 nia P-TEFb-dependens in vitro transcriptio. Apoptosin inducit in vitro et in vivo in compositione cum BI 894999. |
CPD100910 | SEL120-34A | SEL120-34A potens et selectivus inhibitor CDK8 in AML cellulis activus est cum phosphorylatione serinarum STAT1 et STAT5 ditionum transactionis altae. EL120-34A vetat phosphorylationem STAT1 S727 et STAT5 S726 in cellulis cancri in vitro. Congruenter moderatio STATs- et NUP98-HOXA9 transcriptio dependens observata est ut dominans mechanismus actionis in vivo. |
CPDB1540 | MSC2530818 | MSC2530818 Potens, selectiva, et oretenus Bioavailable CDK8 Inhibitor cum CDK8 IC50 = 2.6 nM; Vaticinium humanum PK: CL ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F> 75%. |
CPDB1574 | CYC-065 | CYC065 secunda generatio est, viva voce inhibitor ATP-competitivus inhibitor CDK2/CDK9 kinases potentiale cum actionibus antineoplasticis et chemoprotecticis. |
CPDB1594 | THZ531 | THZ531 est CDK12 covalens et inhibitor covalens CDK13. Cyclin-kinases dependentes 12 et 13 (CDK12 et CDK13) partes criticas in moderandis transcriptionis gene. |
CPDB1587 | THZ2 | THZ2, analogum THZ1, cum potentia tractandi cancer pectus triplicem negativum (TNBC), est potens et selectivus CDK7 inhibitor qui instabilitatem THZ1 vivo vincit. IC50: CDK7= 13.9 nM; TNBC cellae = 10 nM |