| CAT # | Inoa Huahana | wehewehe |
| CPD100904 | Voruciclib | ʻO Voruciclib, ka mea i ʻike ʻia ʻo P1446A-05, he mea pale kinase kinase kikoʻī no ka cyclin-dependent kinase 4 (CDK4) me ka hana antineoplastic. Kāohi ʻia ka CDK4 inhibitor P1446A-05 i ka CDK4-mediated G1-S phase transition, ka hopu ʻana i ke kaʻa kaʻa a me ka pale ʻana i ka ulu ʻana o ka maʻi kanesa. Loaʻa ka serine/threonine kinase CDK4 i loko o kahi paʻakikī me D-type G1 cyclins a ʻo ia ka kinase mua i hoʻāla ʻia ma luna o ka hoʻoulu ʻana i ka mitogenic, e hoʻokuʻu ana i nā cell mai kahi pae kuʻi i ka pae kaʻa kaʻa ulu G1 / S; Ua hōʻike ʻia nā paʻakikī CDK-cyclin i ka phosphorylate i ka retinoblastoma (Rb) transcription factor i ka G1 mua, ka hoʻoneʻe ʻana i ka histone deacetylase (HDAC) a me ka pale ʻana i ka repression transcriptional. |
| CPD100905 | Alvocidib | ʻO Alvocidib kahi pūhui synthetic N-methylpiperidinyl chlorophenyl flavone. Ma keʻano he mea hoʻopaneʻe o ka cyclin-dependent kinase, alvocidib induces cell cycle arrest ma ka pale ʻana i ka phosphorylation of cyclin-dependent kinases (CDKs) a me ka hoʻoponopono iho ʻana i ka cyclin D1 a me D3 hōʻike, ka hopena i ka hopu ʻia ʻana o ka pōʻai cell G1 a me ka apoptosis. He mea hoʻokūkū hoʻokūkū hoʻi kēia mea hana i ka hana adenosine triphosphate. E nānā no nā hoʻokolohua lapaʻau ikaika a i ʻole nā hoʻokolohua lapaʻau pani ʻia me ka hoʻohana ʻana i kēia mea hana. |
| CPD100906 | BS-181 | ʻO BS-181 kahi mea hoʻopaneʻe CDK koho loa no CDK7 me kahi IC(50) o 21 nmol/L. ʻO ka hoʻāʻo ʻana i nā CDK ʻē aʻe a me nā kinase 69 ʻē aʻe i hōʻike ʻia ʻo BS-181 wale nō ke kāohi i ka CDK2 ma nā haʻahaʻa haʻahaʻa haʻahaʻa ma mua o 1 micromol/L, me ka CDK2 i hoʻopaʻa ʻia he 35-fold ka liʻiliʻi (IC(50) 880 nmol/L) ma mua o CDK7. I loko o nā pūnaewele MCF-7, ua kāohi ʻo BS-181 i ka phosphorylation o nā substrates CDK7, hoʻoikaika i ka hopu ʻana o ka cell cycle a me ka apoptosis e pale ai i ka ulu ʻana o nā laina maʻi kanesa, a hōʻike i nā hopena antitumor i vivo. |
| CPD100907 | Riviciclib | ʻO Riviciclib, i kapa ʻia ʻo P276-00, he flavone a me ka cyclin dependent kinase (CDK) inhibitor me ka hana antineoplastic. P276-00 koho a hoʻopaʻa i ka Cdk4/cyclin D1, Cdk1/cyclin B a me Cdk9/cyclin T1, serine/threonine kinases e pāʻani ana i nā kuleana koʻikoʻi i ka hoʻoponopono ʻana i ka pōʻai cell a me ka hoʻonui ʻana o nā kelepona. ʻO ka hoʻopaʻa ʻana i kēia mau kinases e alakaʻi i ka hopu ʻana i ka cell cycle i ka wā o ka hoʻololi ʻana o G1/S, a laila e alakaʻi ana i kahi induction o apoptosis, a me ka pale ʻana i ka hoʻonui ʻana o ka cell tumor. |
| CPD100908 | MC180295 | ʻO MC180295 kahi mea hoʻopiʻi CDK9 koho nui loa (IC50 = 5 nM). (MC180295 he ākea anti-cancer hana in vitro a he mea pono i loko o vivo maʻi 'aʻai kŘkohu. |
| 1073485-20-7 | LDC000067 | ʻO LDC000067 kahi mea hoʻopale CDK9 ikaika a koho. LDC000067 inhibited in vitro transcription in a ATP-competitive and dose-dependent manner. Hōʻike ʻia ka hōʻike ʻana o Gene expression profile o nā cell i mālama ʻia me LDC000067 i kahi hōʻemi koho o nā mRNA pōkole, me nā mea hoʻoponopono koʻikoʻi o ka hoʻonui a me ka apoptosis. ʻO ka loiloi o ka de novo RNA synthesis i manaʻo i kahi kūlana maikaʻi ākea o CDK9. Ma ka pae molecular a me ka cellular level, LDC000067 reproduced effects hiʻona o ka CDK9 inhibition e like me ka hoʻonui ʻana i ka pausing o RNA polymerase II ma nā genes a, ʻo ka mea nui loa, ka hoʻokomo ʻana o ka apoptosis i loko o nā pūnana maʻi maʻi. Kāohi ʻo LDC000067 i ka P-TEFb i hilinaʻi ʻia i ka transcription in vitro. Induces apoptosis in vitro a in vivo i hui pū me BI 894999. |
| CPD100910 | SEL120-34A | ʻO SEL120-34A kahi mea hoʻopale CDK8 ikaika a koho i loko o nā pūnaewele AML me nā kiʻekiʻe o ka serine phosphorylation o STAT1 a me STAT5 transactivation domain. Kāohi ʻo EL120-34A i ka phosphorylation o STAT1 S727 a me STAT5 S726 i loko o nā pūnana maʻi maʻi in vitro. I ka manawa like, ua ʻike ʻia ka hoʻoponopono ʻana o STATs- a me NUP98-HOXA9- hilinaʻi transcription ma ke ʻano he hana mana o ka hana ma vivo. |
| CPDB1540 | MSC2530818 | ʻO MSC2530818 kahi mea hoʻokae CDK8 Potent, Selective, a me ka waha Bioavailable me CDK8 IC50 = 2.6 nM; wānana PK kanaka: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | ʻO CYC065 ka lua o ka hanauna, i loaʻa i ka waha i ka ATP-competitive inhibitor o CDK2/CDK9 kinases me nā hana antineoplastic a me chemoprotective. |
| CPDB1594 | THZ531 | ʻO THZ531 kahi mea hoʻopanee CDK12 a me CDK13 covalent inhibitor. ʻO Cyclin-dependent kinases 12 a me 13 (CDK12 a me CDK13) ke hana koʻikoʻi i ka hoʻoponopono ʻana i ka transcription gene. |
| CPDB1587 | THZ2 | ʻO THZ2, kahi analog o THZ1, me ka hiki ke mālama i ka Triple-negative breast cancer (TNBC), he mea hoʻopaneʻe CDK7 ikaika a koho i lanakila i ka instability o THZ1 in vivo. IC50: CDK7= 13.9 nM; Nā pūnaewele TNBC= 10 nM |
