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 Á¦Ç°¾È³»  ½Å°æ¾àÇР  Cell Biology

Cell Cycle Related Inhibitiors

Cell CycleÀº ¼¼Æ÷ÀÇ Áõ½ÄÀ» À§ÇØ DNA¿Í º¹Á¦¿Í ¼¼Æ÷ºÐ¿­ÀÌ ÀϾ±â±îÁöÀÇ ÀÏ·ÃÀÇ °úÁ¤À¸·Î, Cell CycleÀ» ¿¬±¸Çϴµ¥ ÇÊ¿äÇÑ CDK, Aurora, p53°ü·Ã inhibitor, activator¸¦ ¼Ò°³ÇÕ´Ï´Ù.

TOCRIS
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  • Aurora Kinases

         Aurora kinases´Â ü¼¼Æ÷ºÐ¿­¿¡ ÁßÃßÀûÀÎ ¿ªÇÒÀ» ´ã´çÇϰí ÀÖÀ¸¸ç, Aurora A, Aurora B ±×¸®°í
         Aurora CÀÇ 3°¡Áö isoformÀº °¢°¢ ¼­·Î ´Ù¸¥ ±â´ÉÀ¸·Î ü¼¼Æ÷ ºÐ¿­À» Á¶ÀýÇÕ´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 4291 CCT 137690  Potent pan-Aurora kinase inhibitor 
Inhibitor 3988 Hesperadin hydrochloride Potent Aurora kinase B inhibitor 
Inhibitor 4821 PF 03814735  Aurora kinase A and B inhibitor 
Inhibitor 4584 SNS 314 mesylate  Potent pan-Aurora kinase inhibitor 
Inhibitor 4066 TC-A 2317 hydrochloride  Potent, selective Aurora kinase A inhibitor 
Inhibitor 5286 TC-S 7010  Potent and selective Aurora kinase A inhibitor 
Inhibitor 2458 ZM 447439 Inhibits Aurora kinase B 
Activator 3084 Anacardic acid  Aurora kinase A activator. Also inhibits histone acetyltransferase 

 

  • Cdc25 Phosphatase

          Cdc25´Â cdc25A, B ±×¸®°í C 3°¡Áö isoformÀÌ ÀÖÀ¸¸ç, Cell cycle ÁøÇà¿¡ ÁßÀ翪ÇÒÀ» ÇÕ´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 1867 NSC 663284  Potent, selective Cdc25 phosphatase inhibitor 
Inhibitor 1547 NSC 95397 Selective Cdc25 dual specificity phosphatase inhibitor 

 

  • Cell Cycle Inhibitors

          Cell cycle inhibitor´Â ´Ù¾çÇÑ ¸ÞÄ¿´ÏÁòÀ» ÅëÇØ cell cycle ÁøÇàÀ» ´ÊÃ߰ųª ¸ØÃß°Ô ÇÕ´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 5331 CPI 203 Arrests cell cycle at G1 phase; also BET bromodomain inhibitor 
Other 4406 10058-F4  Arrests cell cycle at G0/G1 
Other 4138 ABT 751  Inhibitor of microtubule polymerization; blocks cell cycle at G2M 
Other 1761 Baicalein  Induces G1 and G2 cell cycle arrest. Also lipoxygenase inhibitor  
Other 5144 CFM 4  CARP-1 mimetic; induces G2/M cell cycle arrest 
Other 1417 Daidzein  Arrests cell cycle in G1 phase 
Other 4761 Plumbagin  Induces G2/M cell cycle arrest; anticancer
Other 5264 Temsirolimus mTOR inhibitor; arrests cell cycle at G1/S 
Other 4282 WYE 687 dihydrochloride  Potent and selective mTOR inhibitor; induces G1 cell cycle arrest 
  • Checkpoint Control Kinases

          Checkpoint control kinases´Â Cell Cycle Àü¹Ý¿¡ °ÉÃÄ ÁøÇàÀÌ ±ÔÄ¢ÀûÀ¸·Î µÉ ¼ö ÀÖµµ·Ï Á¶ÀýÇϸç, ÇÊ¿äÇÑ
          ¾Õ ´Ü°è°¡ ¿Ï·áµÇÁö ¾ÊÀ¸¸é ´ÙÀ½   ´Ü°è·Î ÁøÇàµÉ ¼ö ¾ø½À´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 3994 AZ 3146 Potent and selective monopolar spindle 1 (Mps1) inhibitor 
Inhibitor 3544 KU 55933  Potent and selective ATM kinase inhibitor 
Inhibitor 3034 NSC 109555 ditosylate  Selective Chk2 inhibitor 
Inhibitor 3712 NU 7441  Potent and selective DNA-PK inhibitor 
Inhibitor 2694 PD 407824  Selective inhibitor of Chk1 and Wee1 
Inhibitor 4277 PF 477736 Selective Chk1 inhibitor 
Inhibitor 2560 SB 218078  Inhibitor of checkpoint kinase 1 (Chk1) 
Inhibitor 3038 TCS 2312  Potent Chk1 inhibitor 
Other 4502 DIM  Activates Chk2; induces G2/M cell cycle arrest 
Other 4763 Pyridostatin pentahydrochloride  Stabilizes G-quadruplexes; induces DNA damage and cell cycle arrest 

 

  • Cyclin-Dependent Protein Kinase

          Cdks´Â cell-cycle control system¿¡¼­ °¡Àå Áß¿äÇÑ ¿ä¼ÒÁßÀÇ Çϳª·Î, Cyclin´Ü¹éÁú°ú °áÇÕÇÏ¿© cyclin D
          º¹ÇÕü¸¦ Çü¼ºÇÏ¿© ¼¼Æ÷Áֱ⸦ Á¶ÀýÇÒ ¼ö ÀÖÀ¸¸ç, 12°¡Áö CDK À¯ÀüÀÚ°¡ ÀÖÀ¸³ª, Cdk1, -2, -3, -4, -6 5°¡Áö
          À¯ÀüÀÚ¸¸ÀÌ Á÷Á¢ÀûÀ¸·Î ¼¼Æ÷Áֱ⸦ Á¶ÀýÇÏ´Â ´É·ÂÀÌ ÀÖ½À´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 3610 (R)-DRF053 dihydrochloride  Dual cdk1/cdk5 inhibitor. Also inhibits CK1 
Inhibitor 1902 [Ala92]-p16 (84-103)  Cyclin-dependent kinase inhibitor 
Inhibitor 1532 10Z-Hymenialdisine  Pan kinase inhibitor; potently inhibits Cdk1, Cdk2, Cdk3 and Cdk5 
Inhibitor 2457 Arcyriaflavin A  Potent cdk4/cyclin D1 and CaM Kinase II inhibitor. Antiviral agent (anti-HCMV) 
Inhibitor 3094 Flavopiridol hydrochloride  Cyclin-dependent kinase inhibitor 
Inhibitor 2152 NSC 625987   Cyclin-dependent kinase 4 (cdk4) inhibitor 
Inhibitor 3135 NU 2058 Cdk1 and cdk2 inhibitor 
Inhibitor 4786 PD 0332991 isethionate  Potent, selective Cdk4/6 inhibitor; brain penetrant 
Inhibitor 4181 Ro 3306  Cyclin-dependent kinase (cdk) 1 inhibitor 
Inhibitor 2907 SU 9516   Potent cdk2 inhibitor 

 

  • Mitosis

          ü¼¼Æ÷ºÐ¿­Àº ÇϳªÀÇ ¸ð¼¼Æ÷·ÎºÎÅÍ µÎ °³ÀÇ µþ¼¼Æ÷¸¦ ¸¸µé¾î³»¸ç, °£±â, Àü±â, ÀüÁß±â, Èıâ, ¸»±â 5´Ü°è·Î ÁøÇàµË´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 5399 BTB1 Selective and ATP-competitive Kif18A inhibitor 
Inhibitor 1364 Colchicine   Inhibitor of tubulin 
Inhibitor 1495 Combretastatin A4  Inhibits tubulin polymerization. Antitumor, antiangiogenic and antimetastatic 
Inhibitor 1643 D-64131  Inhibitor of tubulin polymerization. Antitumor in vivo 
Inhibitor 5261 Dimethylenastron Inhibitor of mitotic motor kinesin Eg5; antimitotic 
Inhibitor 1228 Nocodazole  Microtubule inhibitor 
Inhibitor 1232 Wortmannin  Potent inhibitor of PLK1. Also inhibitor of PI 3-kinase 
Other 3502 Epothilone B  Microtubule stabilization agent; promotes G2-M cell cycle arrest 
Other 3728 Indibulin  Microtubule destabilizer 
Other 3551 INH1  Hec1 inhibitor; causes arrest of mitosis 
Other 1097 Taxol  Promotes assembly and inhibits disassembly of microtubules 

 

  • p53

          p53Àº ¼¼Æ÷ÀÇ ¹«ºÐº°ÇÑ Áõ½Ä°ú µ¹¿¬º¯À̸¦ ¸·´Â transcription factor·Î, p53Àº ATM, ATR, Chk1, MAPKs¿¡ ÀÇÇÑ
          ÀλêÈ­µî ¿©·¯ ¸ÞÄ¿´ÏÁò¿¡ ÀÇÇØ Ȱ¼ºÈ­µË´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 2936 NSC 66811  MDM2 inhibitor. Disrupts MDM2-p53 interaction 
Inhibitor 3843 Cyclic Pifithrin-α hydrobromide  p53 inhibitor 
Inhibitor 2653 Pifithrin-μ  Inhibitor of p53-mitochondrial binding 
Inhibitor 2443 RITA  p53-MDM2 interaction inhibitor; antitumor 
Activator 2185 NSC 146109 hydrochloride  Cell-permeable, genotype-selective antitumor agent; activates p53-dependent transcription
Activator 3365 Tenovin-1  Activates p53 transcriptional activity 
Activator 3356 WR 1065  p53 activator. Also ROS scavenger 
Other 3023 CP 31398 dihydrochloride  p53-stabilizing agent 

 

  • Poly(ADP-ribose) Polymerase

          PARP´Â NAD¸¦ ±âÁú·Î histone µîÀÇ ÇÙ ´Ü¹éÁú¿¡ ºÎ°¡µÇ´Â polymer·Î¼­, ¿°»öÁú ±¸Á¶ÀÇ Á¦¾î¿Í DNA º¹±¸¿¡
          °ü¿©ÇÏ´Â °ÍÀ¸·Î ¾Ë·ÁÁ® ÀÖ½À´Ï´Ù.

Function Cat. No. Product Name  Activity
Inhibitor 0788 3-Aminobenzamide  PARP inhibitor 
Inhibitor 3735 BYK 49187 PARP-1 and PARP-2 inhibitor 
Inhibitor 2192 4-HQN   PARP inhibitor 
Inhibitor 4514 JW 55  Tankyrase inhibitor; inhibits canonical Wnt signaling 
Inhibitor 5084 MN 64 Potent and selective tankyrase inhibitor 
Inhibitor 3736 UPF 1069  PARP-2 inhibitor 
Inhibitor 3748 XAV 939  Tankyrase inhibitor; inhibits Wnt signaling