| CAT # | Khoom npe | Kev piav qhia |
| PIB 100904 | Voruciclib | Voruciclib, tseem hu ua P1446A-05, yog ib qho protein kinase inhibitor tshwj xeeb rau cyclin-dependent kinase 4 (CDK4) uas muaj peev xwm ua haujlwm antineoplastic. CDK4 inhibitor P1446A-05 tshwj xeeb inhibits CDK4-mediated G1-S theem hloov pauv, ntes cell cycling thiab inhibiting mob qog noj ntshav. Lub serine / threonine kinase CDK4 muaj nyob rau hauv ib qho nyuaj nrog D-hom G1 cyclins thiab yog thawj kinase los ua kom tau raws li mitogenic stimulation, tso hlwb los ntawm ib tug quiescent theem mus rau lub G1 / S loj hlob cycling theem; CDK-cyclin complexes tau pom tias phosphorylate lub retinoblastoma (Rb) transcription factor nyob rau hauv thaum ntxov G1, displacing histone deacetylase (HDAC) thiab thaiv transcriptional repression. |
| PIB 100905 | Alvocidib | Alvocidib yog ib qho hluavtaws N-methylpiperidinyl chlorophenyl flavone compound. Raws li tus inhibitor ntawm cyclin-dependent kinase, alvocidib induces cell voj voog ntes los ntawm kev tiv thaiv phosphorylation ntawm cyclin-dependent kinases (CDKs) thiab los ntawm down-regulating cyclin D1 thiab D3 qhia, ua rau G1 cell voj voog ntes thiab apoptosis. Tus neeg sawv cev no kuj yog ib qho kev sib tw inhibitor ntawm adenosine triphosphate kev ua haujlwm. Tshawb xyuas cov kev sim tshuaj kho mob lossis kaw qhov kev sim tshuaj uas siv tus neeg sawv cev no. |
| PIB 100906 | IB-181 | BS-181 yog ib qho kev xaiv CDK inhibitor rau CDK7 nrog IC (50) ntawm 21 nmol / L. Kev ntsuam xyuas ntawm lwm cov CDKs thiab lwm yam 69 kinases pom tau tias BS-181 tsuas yog inhibited CDK2 ntawm cov concentrations qis dua 1 micromol/L, nrog CDK2 raug inhibited 35-fold tsawg zog (IC(50) 880 nmol/L) dua CDK7. Hauv MCF-7 hlwb, BS-181 inhibited phosphorylation ntawm CDK7 substrates, txhawb nqa lub voj voog ntawm tes thiab apoptosis txhawm rau tiv thaiv kev loj hlob ntawm cov kab mob qog noj ntshav, thiab pom cov teebmeem antitumor hauv vivo. |
| PAB 100907 | Riviciclib | Riviciclib, tseem hu ua P276-00, yog ib qho flavone thiab cyclin dependent kinase (CDK) inhibitor uas muaj peev xwm ua haujlwm antineoplastic. P276-00 xaiv khi rau thiab inhibits Cdk4/cyclin D1, Cdk1/cyclin B thiab Cdk9/cyclin T1, serine/threonine kinases uas ua lub luag haujlwm tseem ceeb hauv kev tswj ntawm lub voj voog ntawm tes thiab kev loj hlob ntawm tes. Inhibition ntawm cov kinases ua rau lub voj voog ntawm tes raug ntes thaum lub sij hawm hloov G1 / S, yog li ua rau induction ntawm apoptosis, thiab inhibition ntawm qog cell proliferation. |
| PIB 100908 | TIAB SA 180295 | MC180295 yog ib qho kev xaiv CDK9 inhibitor (IC50 = 5 nM). (MC180295 muaj kev tiv thaiv kabmob kheesxaws hauv vitro thiab muaj txiaj ntsig zoo hauv vivo cov qauv mob qog noj ntshav. Tsis tas li ntawd, CDK9 inhibition sensitizes rau lub cev tiv thaiv kab mob inhibitor α-PD-1 hauv vivo, ua rau nws lub hom phiaj zoo rau kev kho mob qog noj ntshav. |
| 1073485-20-7 | LDC000067 | LDC000067 yog ib qho muaj zog thiab xaiv CDK9 inhibitor. LDC000067 inhibited hauv vitro transcription nyob rau hauv ATP-kev sib tw thiab koob tshuaj-raws li. Gene qhia profileing ntawm cov hlwb kho nrog LDC000067 pom tau tias txo qis ntawm mRNAs luv luv, suav nrog cov tswj hwm tseem ceeb ntawm kev loj hlob thiab apoptosis. Kev tshuaj xyuas ntawm de novo RNA synthesis qhia txog lub luag haujlwm zoo ntawm CDK9. Ntawm qib molecular thiab cellular, LDC000067 rov tsim cov yam ntxwv ntawm CDK9 inhibition xws li txhim kho kev ncua ntawm RNA polymerase II ntawm cov noob thiab, qhov tseem ceeb tshaj, induction ntawm apoptosis hauv cov qog nqaij hlav cancer. LDC000067 inhibits P-TEFb-nyob rau hauv vitro transcription. Induces apoptosis hauv vitro thiab hauv vivo ua ke nrog BI 894999. |
| PIB 100910 | SEL120-34A | SEL120-34A yog lub zog thiab xaiv CDK8 inhibitor nquag ua haujlwm hauv AML hlwb nrog qib siab ntawm serine phosphorylation ntawm STAT1 thiab STAT5 transactivation domains. EL120-34A inhibits phosphorylation ntawm STAT1 S727 thiab STAT5 S726 hauv cov qog nqaij hlav hauv vitro. Raws li txoj cai, kev tswj hwm ntawm STATs- thiab NUP98-HOXA9- nyob ntawm qhov kev hloov pauv tau raug pom tias yog qhov tseem ceeb ntawm kev ua haujlwm hauv vivo. |
| TIAB SA 1540 | MSC2530818 | MSC2530818 yog lub peev xwm, xaiv, thiab Orally Bioavailable CDK8 Inhibitor nrog CDK8 IC50 = 2.6 nM; Tib neeg PK kwv yees: Cl ~ 0.14 L / H / Kg; t1/2 ~ 2.4h; F> 75%. |
| TIAB SA 1574 | TSI-065 | CYC065 yog ib tiam thib ob, hais lus muaj ATP-kev sib tw inhibitor ntawm CDK2/CDK9 kinases uas muaj peev xwm antineoplastic thiab chemoprotective kev ua ub no. |
| TIAB SA 1594 | TIAB SA 531 | THZ531 yog covalent CDK12 thiab CDK13 covalent inhibitor. Cyclin-dependent kinases 12 thiab 13 (CDK12 thiab CDK13) ua lub luag haujlwm tseem ceeb hauv kev tswj hwm ntawm noob caj noob ces. |
| TIAB SA 1587 | THZ 2 | THZ2, ib qho analog ntawm THZ1, nrog lub peev xwm los kho Triple-negative mis cancer (TNBC), nws yog lub zog thiab xaiv CDK7 inhibitor uas kov yeej qhov tsis ruaj khov ntawm THZ1 hauv vivo. IC50: CDK7 = 13.9 nM; TNBC cells = 10 nM |
