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          阿拉丁小分子抑制劑、激動劑、拮抗劑--DNA損傷/DNA修復信號通路

          來源: 上海阿拉丁生化科技股份有限公司   2020-11-27   訪問量:587評論(0)

          ">K126884KU-55933 (ATM Kinase Inhibitor)≥98%587871-26-95mg,25mg,100mg無細胞ATM12.9 nM2.2 nMK127121KU-60019≥98%925701-49-15mg,25mg,100mg無細胞ATM6.3 nMV125220VE-821≥98%1232410-49-95mg,25mg,100mg無細胞ATR13 nM26 nMW100984Wortmannin98%19545-26-75mg,10mg,25mg無細胞PI3K3 nMDNA-PK/ATM16 nMDNA-PK/ATM150 nMT129646Torin 2≥98%1223001-51-15mg,10mg,50mgp53−/− MEFs細胞系mTOR0.25 nMPC3細胞系ATM/ATR/DNA-PK 28 nMATM/ATR/DNA-PK 35 nMATM/ATR/DNA-PK 118 nMC128014CP-466722≥98%1080622-86-15mg,25mgATM410 nME125288ETP-46464≥99%1345675-02-610mg,50mgATR25 nMC129735CGK 733≥99%905973-89-95mg,10mg,50mgATM200 nMATR200 nMA125603AZ20≥98%1233339-22-45mg,10mg,50mg無細胞ATR5 nMS117968五味子乙素分析標準品,>98%61281-37-625mg,100mgATR7.25 μMC129284磷酸氯喹≥99%50-63-55g,10g,25g,100g,500g ATM

          *PARP

          項目號產品名稱規格CAS包裝細胞靶點IC50KiEC50
          O126162Olaparib (AZD2281, Ku-0059436)≥98%763113-22-010mg,25mg,100mg,250mg,1g,5gPARP15 nM
          PARP21 nM
          V127105Veliparib≥99%912444-00-910mg,50mg,250mg無細胞PARP15.2 nM
          PARP22.9 nM
          R129879Rucaparib (AG-014699,PF-01367338)≥99%459868-92-95mg,10mg,50mg PARP1.4 nM
          B125751Iniparib (BSI-201)≥98%160003-66-710mg,50mg,250mg
          B127705BMN 673≥98%1207456-01-610mg,50mg
          A125467AG14361≥98%328543-09-55mg,10mg,50mg無細胞PARP1<5 nM
          A1072073-氨基苯甲酰胺98%3544-24-91g,5g,25g,100gCHO細胞PARP<50 nM
          P129886PJ34 HCl≥97%344458-15-75mg,25mg,100mg PARP 20 nM
          M127627MK-4827 (Niraparib)98%1038915-60-410mg,50mg,100mgPARP1 3.8 nM
          PARP22.1 nM
          U129885UPF 1069≥98%1048371-03-410mg,50mgPARP18.0 μM
          PARP20.3 μM
          A127274AZD2461≥98%1174043-16-35mg,25mg,100mg PARP
          H1571724-羥基喹唑啉≥98.0%(HPLC)491-36-15g,25g,100g
          B110551苯甲酰胺99%55-21-025g,100g,500g,2.5kg PARP3.3 μM
          B110552苯甲酰胺AR,98%55-21-025g,100g,500g PARP3.3 μM
          B118608苯甲酰胺99.5%,升華純化55-21-05g,25gPARP3.3 μM
          P138238吡啶酰胺≥98.0%(HPLC)1452-77-35g,25g,100g PARP95 μM  

          *DNA/RNA合成

          項目號產品名稱規格CAS包裝細胞靶點IC50KiKd
          G120180鹽酸吉西他濱98%122111-03-910mg,50mg,250mg,1g,5g,25gPANC1細胞DNA合成50 nM
          MIAPaCa2細胞40 nM
          BxPC3細胞18 nM
          Capan2細胞12 nM
          P129841Pemetrexed≥99%150399-23-850mg,250mg無細胞TS1.3 nM
          DHFR7.2 nM
          GARFT65 nM
          C110682卡鉑98%41575-94-4100mg,250mg,1g,5g
          P124220噴司他丁98%(HPLC)53910-25-15mg,25mg
          F122998氟達拉濱98%21679-14-150mg,250mg,1g,5g
          O124003奧沙利鉑99%61825-94-325mg,100mg,500mg
          C127663CX-5461≥98%1138549-36-65mg,25mg,100mgHCT-116細胞rRNA合成142 nM
          A375細胞
          MIA PaCa-2細胞
          F1001495-氟尿嘧啶99%51-21-81g,5g,25g,100g,500g
          C124969Capecitabine≥99%154361-50-9250mg,1g,5g,25g
          F122999單磷酸氟達拉濱99%75607-67-925mg,100mg,500mg
          C126447Cidofovir≥98%113852-37-225mg,100mg
          C111218阿糖胞苷98%147-94-41g,5g,25g,100g
          G127944Gemcitabine≥99%95058-81-450mg,100mg,250mg,1g,5g,25g
          D129529Daptomycin≥98%103060-53-310mg,50mg,100mg,1g
          C129833Cladribine≥98%4291-63-810mg,50mg,100mg,250mg,25gU266, RPMI8226MM1.S細胞腺苷脫氨酶2.43 μM
          U266, RPMI8226MM1.S細胞0.75 μM
          U266, RPMI8226MM1.S細胞0.18 μM
          R129835Raltitrexed≥98%112887-68-010mg,50mg,100mg
          C102625克羅拉濱99%123318-82-15mg,20mg,25mg,100mg,500mg Ribonucleotide reductase65 nM
          I123381異環磷酰胺藥用級3778-73-250mg,250mg,1g,5g
          I123242異環磷酰胺98%3778-73-21g,5g,25g
          N129848NSC 207895≥99%58131-57-01mg,5mg,10mg,50mg MDMX2.5 μM
          D129847Dacarbazine≥98%4342-03-41g,5g,25g
          H106352羥基脲98%127-07-11g,5g,25g,100g
          F1107325-氟-2'-脫氧尿苷99%50-91-9100mg,250mg,500mg,1g,5g,25g
          M1268586-巰基嘌呤 (6-MP)≥99%50-44-250mg,250mg,1g,5g,25g,100g
          M129842Mizoribine≥98%50924-49-710mg,50mg,100mg,250mg
          M104154甲萘醌98%58-27-55g,25g,100g,250g,500g
          C153374卡莫氟>98.0%(HPLC)61422-45-55g,25g
          F129607Fidaxomicin≥99%873857-62-65mg,50mg,100mg,250mg
          M109874甲硝唑99%443-48-15g,25g,100g,500g
          M109873甲硝唑分析標準品,>99.8%(GC)443-48-15g,25g,100g
          T129222Trifluridine≥98%70-00-850mg,100mg,250mg,1g
          R126176Rifaximin≥97%80621-81-4250mg,1g,5g,25g
          P129854Procarbazine HCl≥98%366-70-150mg,250mg,1g
          A170956阿糖腺苷99%5536-17-41g,5g,25g
          R105455Rifampicin97%13292-46-1250mg,1g,5g,25g,100g
          C129367Clevudine≥99%163252-36-610mg,50mg
          M113888氮芥鹽酸鹽98%55-86-75g,25g
          T125377FT-207 (NSC 148958)≥98% (HPLC)17902-23-75g,25g,100g
          N129652Nedaplatin≥99%95734-82-010mg,50mg,250mg DNA合成94 μM
          M102403Mupirocin95%12650-69-025mg,50mg,100mg,250mg,1g
          E106318維生素D298%50-14-61g,5g,25gpol A123 mM
          A1185591-(1-金剛烷基)乙基胺鹽酸鹽99%1501-84-41g,5g,25g,100g
          M1118206-巰基嘌呤 一水合物98%6112-76-11g,5g,25g
          M1118196-巰基嘌呤 一水合物99.50%6112-76-11g,5g,25g
          P101249補骨脂素98%66-97-725mg,100mg,500mg
          P101248補骨脂素分析標準品,≥98%66-97-720mg
          C103233鹽酸環胞苷98%10212-25-61g,5g,25g
          N1248377-**吲哚-2-羧酸≥97%(HPLC)6960-45-8250mg,1g,5gAPE1~3 μM
          N159515鹽酸尼莫司汀>98.0%(HPLC)(T)55661-38-6250mg,1g
          V119467阿糖腺苷一水合物99%24356-66-91g,5g
          P127282Sofosbuvir≥99%1190307-88-05mg,25mg,100mg
          C132260Carmustine≥98%154-93-825mg,100mg,500mg,25g
          Y127218 YK-4-279≥98%1037184-44-310mg,50mg,100mg
          M101153佛手苷內酯>98.0%(GC)484-20-850mg,250mg,1g,5g
          M101152佛手苷內酯分析標準品,>98.0%(GC)484-20-820mg
          M1584395-甲氧基黃酮>98.0%(GC)42079-78-7200mg,1g,2.5g,5g
          O131612噁喹酸98%14698-29-45g,25g
          O114347噁喹酸分析標準品14698-29-4250mg
          C139195鹽酸阿糖胞苷≥99%69-74-9250mg,1g,5g,25g <, /td>
          B139600滅瘟素 S 鹽酸鹽≥96%3513-03-910mg,25mg,100mg
          C154015氯氨布西>98.0%305-03-350mg,200mg,1g,5g
          T102749異*尿酸三縮水甘油酯98%2451-62-925g,100g,250g,500g
          F129839Flupirtine maleate≥99%75507-68-510mg,25mg,100mg,1g
          P128017Pyridostatin-1085412-37-85mg,10mg,25mg,50mg,100mg無細胞G-quadruplexe490 nM
          B107423硫酸博來霉素1.5-2.0 units/mg9041-93-45mg,25mg,100mg
          P166509嘌呤98%120-73-01g,5g
          T127425Temozolomide≥98% (HPLC)85622-93-1250mg,500mg,1g,5g,25g,100g
          B124707Bendamustine HCl≥98%(HPLC)3543-75-7100mg,500mg
          L123247洛莫司汀98%13010-47-450mg,250mg,1g
          B1107315-溴-2'-脫氧尿苷(BUdR)99%59-14-3250mg,1g,5g,25g
          G104274鳥嘌呤99%73-40-55g,25g,100g,250g,500g
          D1003632’-脫氧尿苷99%951-78-01g,5g,25g
          A1295678-氮雜鳥嘌呤≥95%134-58-71g,5g,25g
          T104771β-胸苷99%50-89-51g,5g,25g,100g
          A108805腺嘌呤≥99.5%(HPLC)73-24-55g,25g,100g,250g
          A108804腺嘌呤98%73-24-525g,100g,500g,2.5kg
          C101487胞苷-5'-三磷酸二鈉鹽(CTP)95%36051-68-01g,5g,25g
          C101008胞苷-5'磷酸(5'-CMP)99%63-37-61g,5g
          C100916胞苷-5'磷酸98%63-37-61g,5g,25g
          U1003655’-三磷酸尿苷三鈉(UTP)99%19817-92-625mg,100mg,500mg,1g,5g
          N191760N6-甲基腺苷98%1867-73-8250mg,1g
          U108811尿嘧啶核苷99%,用于細胞培養58-96-85g,25g
          U108810尿嘧啶核苷99%58-96-85g,25g,100g
          T108392胸腺嘧啶99%,用于細胞培養65-71-45g,25g
          T108391胸腺嘧啶99%65-71-45g,25g,100g,500g     

          *Sirtuin

          項目號產品名稱規格CAS包裝細胞靶點IC50EC50
          E129892EX 527 (Selisistat)≥98%49843-98-35mg,10mg,50mg無細胞SIRT138 nM
          N108087煙酰胺用于細胞和昆蟲細胞培養,≥99.5% (HPLC)98-92-0100g,500g
          N108086煙酰胺≥99.5%(HPLC)98-92-0100g,250g,500g
          N105043煙酰胺分析標準品,≥99.8%98-92-01g
          N105042煙酰胺99%98-92-0100g,500g
          S129890SRT1720≥98%1001645-58-45mg,10mg,50mg無細胞SIRT10.16 μM
          S140425丹酚酸 B分析標準品121521-90-210mg
          S123658丹酚酸 B≥94%(HPLC)121521-90-25mg,25mg
          Q111274槲皮素95%117-39-51g,10g,50g,250g PI3Kγ2.4 μM
          Q111273槲皮素分析標準品,≥98.5%117-39-520mgPI3Kδ3.0 μM
          Q118458槲皮素,二水分析標準品,≥98%(HPLC)6151-25-320mg
          Q104838槲皮素,二水97%6151-25-35g,10g,25g,50g,100g,250g,500g   

          *Topoisomerase

          項目號產品名稱規格CAS包裝細胞靶點IC50Ki
          D107159鹽酸阿霉素98%25316-40-925mg,100mg,250mg,500mg,1g,5g Topo II
          E121713Etoposide98%33419-42-0100mg,250mg,500mg,1g,5g Topo II
          C111282(S)-(+)-喜樹堿97%7689-03-4100mg,250mg,1g,5g Topo I 0.68 μM
          C111281(S)-(+)-喜樹堿分析標準品,≥98%7689-03-420mgTopo I 0.68 μM
          T294611鹽酸拓撲替康98%119413-54-650mg,250mg無細胞Topo I (MCF-7 Luc細胞)13 nM
          Topo I (DU-145 Luc細胞)2 nM
          T103153鹽酸拓撲替康分析標準品,≥99%(HPLC)119413-54-610mg,50mg無細胞Topo I (MCF-7 Luc細胞)13 nM
          Topo I (DU-145 Luc細胞)2 nM
          I129863Idarubicin HCl≥98%57852-57-01mg,5mg,10mg,50mg無細胞Topo II (MCF-7 cells) 3.3 ng/mL
          R139432魯比特康≥98.0%(HPLC)91421-42-025mg,100mg
          E122334鹽酸表柔比星≥98% (HPLC)56390-09-15mg,25mg
          M129460Mitoxantrone dihydrochloride≥97%70476-82-310mg,50mg,250mg,1g
          D122335鹽酸佐柔比星>90%23541-50-610mg,50mg,250mg無細胞DNA合成0.02 μM
          M129861Moxifloxacin HCl≥99%186826-86-850mg,100mg,500mg,1g,5g,25g
          I129860Irinotecan HCl Trihydrate≥98%136572-09-3100mg,250mg,500mg,1g
          E1101287-乙基-10羥基喜樹堿98%86639-52-3100mg,500mg,1g,5g Topo I
          A126932Amonafide≥98%69408-81-710mg,50mg,250mg
          T125922Teniposide≥98%29767-20-220mg,25mg,100mg
          G129827Gatifloxacin≥98%112811-59-31g,5g,10g,25g
          D129340Dexrazoxane HCl (ICRF-187, ADR-529)≥99%149003-01-010mg,50mg,250mg Topo II
          G106672金雀異黃酮分析標準品,≥98%446-72-020mg,1g,5gNIH-3T3細胞EGFR12μM
          topo II19 μM
          G106673金雀異黃酮97%446-72-0100mg,500mg,1g,5g,25gNIH-3T3細胞EGFR12μM
          topo II19 μM
          L157745Levofloxacin>98.0%(HPLC)100986-85-45g,25g,100g,500g
          P129867Pirarubicin≥97%72496-41-410mg,50mgTopo II
          M139937馬波沙星98%115550-35-11g,5g,25g
          M114260馬波沙星分析標準品115550-35-1100mg
          C129896Ciprofloxacin≥98%85721-33-15g,25g,100g
          N129248Novobiocin Sodium≥95%1476-53-550mg,100mg,500mg,1g,5g
          E194832依諾沙星98%74011-58-81g,5g,25g
          O102014Ofloxacin98%82419-36-11g,5g,25g,100g
          O102012Ofloxacin分析標準品,≥99.0%(HPLC)82419-36-1100mg
          N114262諾氟沙星98%70458-96-71g,5g,25g,100g,500g
          N114261諾氟沙星分析標準品70458-96-7100mg
          E102710鞣花酸96%476-66-41g,5g,25g,100g
          N104920萘啶酮酸98%389-08-25g,25g,100g
          C129430Clinafloxacin≥95%105956-97-650mg,250mg,1g
          P102019培氟沙星99%149676-40-45g,25g,100g
          P102018培氟沙星分析標準品149676-40-4100mgTopo II
          A107930鹽酸胺苯吖啶≥98% (HPLC)54301-15-425mg,100mg
          B129359Balofloxacin98%127294-70-6100mg,500mg
          H1075365-**-8-羥基喹啉97%4008-48-45g,25g,100g
          H196266(S)-10-羥基喜樹堿98%19685-09-7500mg,1g,5g,25g
          H109791(S)-10-羥基喜樹堿分析標準品,98%19685-09-725mg,100mg
          T166659Topotecan hydrochloride hydrate98% (HPLC and enzymatic)123948-87-810mg,20mg,50mg
          B123958白樺脂酸97%472-15-1100mg,1g,5g
          B101534白樺脂酸分析標準品,>98%472-15-120mg
          E1348527-乙基喜樹堿≥96.0%(HPLC)78287-27-150mg,250mg,1g,5g,25g
          F131683氟甲喹≥98.0%42835-25-61g,5g,25g,100g
          F114353氟甲喹分析標準品42835-25-6250mg Topo II15 μM
          ,
          阿拉丁小分子抑制劑、激動劑、拮抗劑--DNA損傷/DNA修復信號通路(上)

          DNA損傷/DNA修復

          人類細胞中的DNA每天會受到數以萬計的外源性損傷(化學污染、紫外線、電離輻射、烷基化/甲基化等引起)和內源性損傷(堿的氧化、烷基化、水解等引起)。損傷后DNA會發生單鏈和雙鏈斷裂,未修復的DNA損傷會導致細胞衰老、凋亡和惡性腫瘤等等。為了避免此類情況,激發了細胞的DNA損傷反應(DDR)。DNA損傷反應(DDR)能夠檢測DNA的損傷并介導其修復,包含DNA損傷、細胞周期停滯、DNA復制調控、DNA損傷修復旁路等一系列通路的調控,以維持基因組的穩定性和細胞活力。異常的DNA損傷反應與衰老、癌癥和免疫疾病有關。

          DNA損傷/DNA修復通路轉導過程

          當DNA受到外源性或內源性損傷后,會發生單鏈和雙鏈斷裂,DNA損傷反應會被激活。

          DNA雙鏈斷裂激活DNA-PK與ATM/ATR激酶。DNA-PK誘導DNA修復,涉及錯配、堿基切除、核苷酸切除修復等多種機制。RPA、Rad51和fanconi貧血蛋白等也可直接用于DNA修復。ATM/ATR激酶經過兩個并行級聯最終將CyclinB-cdc2復合體失活:1)ATM/ATR激酶激活Chk2激酶,Chk2激酶磷酸化并使失活Cdc25,同時也通過Chk1抑制Cdc25,從而阻止cdc2的激活,快速抑制細胞有絲分裂從G2期進入M期。此外,ATR通過刺激Cdk1抑制激酶Wee1來抑制Cyclinb/Cdk1的激活,防止DNA損傷的細胞進入有絲分裂。2)另一級聯反應稍慢,Chk2激酶磷酸化p53,使其從MDM2和MDM4(MdmX)上分離,激活p53下游調節基因,從而抑制CyclinB-cdc2復合體活性或將其從細胞核中排出。p300/PCAF對p53乙;蛇M一步增強其轉錄能力。同時,p53也可誘導細胞凋亡。

          DNA單鏈斷裂后,激活ATR激酶,ATR通過Chk1進一步激活Cdc25A。Cdc25A是一種CDK2激活所需的磷酸酶。CDK2抑制周期素E/A,使有絲分裂無法從G1期進入S期。

          DNA損傷/DNA修復信號通路圖

          產品列表

          *HDAC

          項目號產品名稱規格CAS包裝細胞靶點IC50Ki
          V125336Vorinostat≥99.0%149647-78-9100mg,500mg,1g,5g無細胞HDAC~10 nM
          E125068Entinostat (MS-275)≥98%209783-80-210mg,50mg,100mg,250mg無細胞HDAC10.51 μM
          HDAC31.7 μM
          P125167Panobinostat (LBH589)≥98%404950-80-710mg,50mg無細胞HDAC5 nM
          T129665Trichostatin A≥98%58880-19-65mg,10mg,50mg無細胞HDAC1.8 nM
          M126151Mocetinostat (MGCD0103)≥98%726169-73-95mg,25mg,50mg無細胞HDAC10.15 μM
          B126780Belinostat (PXD101)≥98%414864-00-910mg,50mg,250mg無細胞HDAC27 nM
          R125265Romidepsin (FK228, Depsipeptide)≥98%128517-07-71mg,5mg無細胞HDAC136 nM
          HDAC247 nM
          M127417MC1568≥97%(HPLC)852475-26-410mg,25mg無細胞HDAC100 nM
          T129677Tubastatin A HCl≥98%1310693-92-55mg,10mg,50mg,無細胞HDAC615 nM
          G129672Givinostat (ITF2357)≥95%732302-99-71mg,5mg,10mg,50mg無細胞HD210 nM
          HD1B7.5 nM
          HD1A16 nM
          C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mgHDAC4.4 nM
          EGFR2.4 nM
          HER215.7 nM
          P127910Pracinostat (SB939)≥98%929016-96-65mg,10mg,50mg pan-HDAC40-140 nM
          P126351PCI-34051≥98%950762-95-510mg,50mg無細胞HDAC810 nM
          D127578Droxinostat≥96%99873-43-51mg,5mg,10mg,25mgHDACs 62.47μM
          HDACs 81.46 μM
          P126975PCI-24781 (Abexinostat)≥97%783355-60-21mg,5mg,10mg,50mg HDAC17 nM
          R129686RGFP966≥98%1396841-57-85mg,25mg,100mg無細胞HDAC30.08μM
          A127913AR-42≥99%935881-37-11mg,2mg,5mg,10mg,50mg HDAC30 nM
          A124886Rocilinostat (ACY-1215)≥98%1316214-52-45mg,10mg,50mg無細胞HDAC65 nM
          S1610232-丙戊酸鈉≥98.0%1069-66-55g,25g,100g,500g
          C126432CI-994≥98% 112522-64-210mg,50mg,250mgHDAC10.9 μM
          HDAC20.9 μM
          HDAC31.2 μM
          HDAC8>20 μM
          C126527CUDC-907≥99%1339928-25-41mg,5mg,10mg,50mgPI3Kα19 nM
          HDAC11.7 nM
          HDAC25 nM
          PI3Kα和HDAC31.8 nM
          PI3Kα和HDAC102.8 nM
          S102956丁酸鈉99%,用于生物學156-54-75g,25g,100g,500g
          S102954丁酸鈉98%156-54-725g,100g,250g,500g
          C140600姜黃素≥65%458-37-75g,25g,100gHDAC100 nM
          C110685姜黃素分析標準品458-37-720mgHDAC100 nM
          R127721RG2833≥98%1215493-56-35mg,10mg,25mg,50mg,100mg無細胞HDAC160 nM
          HDAC350 nM
          S125104Scriptaid≥99%287383-59-91mg,5mg
          V298968丙戊酸≥98.0%99-66-125ml,100ml,500ml HDAC10.4 mM
          T125086Tasquinimod≥99%254964-60-85mg,10mg,50mg HDAC4
          C168062Crotonoside95% (HPLC)1818-71-95mg,10mg,25mgFLT3
          HDAC3/6
          S135494軟木肟酸95%38937-66-51g,5gHDAC10.25 μM
          HDAC30.3 μM
          S161350斯普利特麻一辛>98.0%(GC)5690-03-9200mg,1gSir2p60 μM
          B1519134-聯苯磺酰氯>98.0%(GC)1623-93-45g,25g,100g
          P115736小白菊內酯分析標準品,≥98%20554-84-120mg   

          *ATM/ATR

          項目號產品名稱規格CAS包裝細胞靶點IC50KiEC50
          B126286BEZ235≥99%915019-65-725mg,100mg,1g無細胞p110α4 nM
          p110γ5 nM
          p110δ7 nM
          p110β 75 nM
          mTOR(p70S6K)6 nM
          3T3TopBP1-ER 細胞ATR21 nM
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