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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂--DNA损伤/DNA修复信号通路

阿拉丁小分子抑制剂、激动剂、拮抗剂--DNA损伤/DNA修复信号通路

发布时间:2020-11-27

阿拉丁小分子抑制剂、激动剂、拮抗剂--DNA损伤/DNA修复信号通路(上)

DNA损伤/DNA修复

       人类细胞中的DNA每天会受到数以万计的外源性损伤(化学污染、紫外线、电离辐射、烷基化/甲基化等引起)和内源性损伤(碱的氧化、烷基化、水解等引起)。损伤后DNA会发生单链和双链断裂,未修复的DNA损伤会导致细胞衰老、凋亡和恶性肿瘤等等。为了避免此类情况,激发了细胞的DNA损伤反应(DDR)。DNA损伤反应(DDR)能够检测DNA的损伤并介导其修复,包含DNA损伤、细胞周期停滞、DNA复制调控、DNA损伤修复旁路等一系列通路的调控,以维持基因组的稳定性和细胞活力。异常的DNA损伤反应与衰老、癌症和免疫疾病有关。

DNA损伤/DNA修复通路转导过程

       当DNA受到外源性或内源性损伤后,会发生单链和双链断裂,DNA损伤反应会被激活。

       DNA双链断裂激活DNA-PK与ATM/ATR激酶。DNA-PK诱导DNA修复,涉及错配、碱基切除、核苷酸切除修复等多种机制。RPA、Rad51和fanconi贫血蛋白等也可直接用于DNA修复。ATM/ATR激酶经过两个并行级联最终将CyclinB-cdc2复合体失活:1)ATM/ATR激酶激活Chk2激酶,Chk2激酶磷酸化并使失活Cdc25,同时也通过Chk1抑制Cdc25,从而阻止cdc2的激活,快速抑制细胞有丝分裂从G2期进入M期。此外,ATR通过刺激Cdk1抑制激酶Wee1来抑制Cyclinb/Cdk1的激活,防止DNA损伤的细胞进入有丝分裂。2)另一级联反应稍慢,Chk2激酶磷酸化p53,使其从MDM2和MDM4(MdmX)上分离,激活p53下游调节基因,从而抑制CyclinB-cdc2复合体活性或将其从细胞核中排出。p300/PCAF对p53乙酰化可进一步增强其转录能力。同时,p53也可诱导细胞凋亡。

       DNA单链断裂后,激活ATR激酶,ATR通过Chk1进一步激活Cdc25A。Cdc25A是一种CDK2激活所需的磷酸酶。CDK2抑制周期素E/A,使有丝分裂无法从G1期进入S期。

DNA损伤/DNA修复信号通路图

产品列表

   *HDAC

项目号产品名称规格CAS包装细胞靶点IC50Ki
V125336Vorinostat≥99.0%149647-78-9100mg,500mg,1g,5g无细胞HDAC~10 nM
E125068Entinostat (MS-275)≥98%209783-80-210mg,50mg,100mg,250mg无细胞HDAC10.51 μM
HDAC31.7 μM
P125167Panobinostat (LBH589)≥98%404950-80-710mg,50mg无细胞HDAC5 nM
T129665Trichostatin A≥98%58880-19-65mg,10mg,50mg无细胞HDAC1.8 nM
M126151Mocetinostat (MGCD0103)≥98%726169-73-95mg,25mg,50mg无细胞HDAC10.15 μM
B126780Belinostat (PXD101)≥98%414864-00-910mg,50mg,250mg无细胞HDAC27 nM
R125265Romidepsin (FK228, Depsipeptide)≥98%128517-07-71mg,5mg无细胞HDAC136 nM
HDAC247 nM
M127417MC1568≥97%(HPLC)852475-26-410mg,25mg无细胞HDAC100 nM
T129677Tubastatin A HCl≥98%1310693-92-55mg,10mg,50mg,无细胞HDAC615 nM
G129672Givinostat (ITF2357)≥95%732302-99-71mg,5mg,10mg,50mg无细胞HD210 nM
HD1B7.5 nM
HD1A16 nM
C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mg
HDAC4.4 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无细胞HDAC810 nM
D127578Droxinostat≥96%99873-43-51mg,5mg,10mg,25mg
HDACs 62.47μM
HDACs 81.46 μM
P126975PCI-24781 (Abexinostat)≥97%783355-60-21mg,5mg,10mg,50mg
HDAC1
7 nM
R129686RGFP966≥98%1396841-57-85mg,25mg,100mg无细胞HDAC30.08μM
A127913AR-42≥99%935881-37-11mg,2mg,5mg,10mg,50mg
HDAC30 nM
A124886Rocilinostat (ACY-1215)≥98%1316214-52-45mg,10mg,50mg无细胞HDAC65 nM
S1610232-丙戊酸钠≥98.0%1069-66-55g,25g,100g,500g



C126432CI-994≥98% 112522-64-210mg,50mg,250mg
HDAC10.9 μM
HDAC20.9 μM
HDAC31.2 μM
HDAC8>20 μM
C126527CUDC-907≥99%1339928-25-41mg,5mg,10mg,50mg
PI3Kα19 nM
HDAC11.7 nM
HDAC25 nM
PI3Kα和HDAC31.8 nM
PI3Kα和HDAC102.8 nM
S102956丁酸钠99%,用于生物学156-54-75g,25g,100g,500g



S102954丁酸钠98%156-54-725g,100g,250g,500g



C140600姜黄素≥65%458-37-75g,25g,100g
HDAC100 nM
C110685姜黄素分析标准品458-37-720mg
HDAC100 nM
R127721RG2833≥98%1215493-56-35mg,10mg,25mg,50mg,100mg无细胞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,25mg
FLT3

HDAC3/6

S135494软木肟酸95%38937-66-51g,5g
HDAC10.25 μM
HDAC30.3 μM
S161350斯普利特麻一辛>98.0%(GC)5690-03-9200mg,1g
Sir2p60 μM
B1519134-联苯磺酰氯>98.0%(GC)1623-93-45g,25g,100g



P115736小白菊内酯分析标准品,≥98%20554-84-120mg



 

*ATM/ATR

项目号产品名称规格CAS包装细胞靶点IC50KiEC50
B126286BEZ235≥99%915019-65-725mg,100mg,1g无细胞p110α4 nM

p110γ5 nM

p110δ7 nM

p110β 75 nM

mTOR(p70S6K)6 nM

3T3TopBP1-ER 细胞ATR21 nM

K126884KU-55933 (ATM Kinase Inhibitor)≥98%587871-26-95mg,25mg,100mg无细胞ATM12.9 nM2.2 nM
K127121KU-60019≥98%925701-49-15mg,25mg,100mg无细胞ATM6.3 nM

V125220VE-821≥98%1232410-49-95mg,25mg,100mg无细胞ATR13 nM26 nM
W100984Wortmannin98%19545-26-75mg,10mg,25mg无细胞PI3K3 nM

DNA-PK/ATM16 nM

DNA-PK/ATM150 nM

T129646Torin 2≥98%1223001-51-15mg,10mg,50mgp53?/? MEFs细胞系mTOR0.25 nM

PC3细胞系ATM/ATR/DNA-PK

28 nM
ATM/ATR/DNA-PK

35 nM
ATM/ATR/DNA-PK

118 nM
C128014CP-466722≥98%1080622-86-15mg,25mg
ATM410 nM

E125288ETP-46464≥99%1345675-02-610mg,50mg
ATR25 nM

C129735CGK 733≥99%905973-89-95mg,10mg,50mg
ATM200 nM

ATR200 nM

A125603AZ20≥98%1233339-22-45mg,10mg,50mg无细胞ATR5 nM

S117968五味子乙素分析标准品,>98%61281-37-625mg,100mg
ATR7.25 μM

C129284磷酸氯喹≥99%50-63-55g,10g,25g,100g,500g
ATM


 

*PARP

项目号产品名称规格CAS包装细胞靶点IC50KiEC50
O126162Olaparib (AZD2281, Ku-0059436)≥98%763113-22-010mg,25mg,100mg,250mg,1g,5g
PARP15 nM

PARP21 nM

V127105Veliparib≥99%912444-00-910mg,50mg,250mg无细胞PARP1
5.2 nM
PARP2
2.9 nM
R129879Rucaparib (AG-014699,PF-01367338)≥99%459868-92-95mg,10mg,50mg
PARP
1.4 nM
B125751Iniparib (BSI-201)≥98%160003-66-710mg,50mg,250mg




B127705BMN 673≥98%1207456-01-610mg,50mg




A125467AG14361≥98%328543-09-55mg,10mg,50mg无细胞PARP1
<5 nM
A1072073-氨基苯甲酰胺98%3544-24-91g,5g,25g,100gCHO细胞PARP<50 nM

P129886PJ34 HCl≥97%344458-15-75mg,25mg,100mg
PARP 

20 nM
M127627MK-4827 (Niraparib)98%1038915-60-410mg,50mg,100mg
PARP1 3.8 nM

PARP22.1 nM

U129885UPF 1069≥98%1048371-03-410mg,50mg
PARP18.0 μM

PARP20.3 μM

A127274AZD2461≥98%1174043-16-35mg,25mg,100mg
PARP


H1571724-羟基喹唑啉≥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%,升华纯化55-21-05g,25g
PARP3.3 μM

P138238吡啶酰胺≥98.0%(HPLC)1452-77-35g,25g,100g
PARP95 μM

 

*DNA/RNA合成

项目号产品名称规格CAS包装细胞靶点IC50KiKd
G120180盐酸吉西他滨98%122111-03-910mg,50mg,250mg,1g,5g,25gPANC1细胞DNA合成50 nM

MIAPaCa2细胞40 nM

BxPC3细胞18 nM

Capan2细胞12 nM

P129841Pemetrexed≥99%150399-23-850mg,250mg无细胞TS
1.3 nM
DHFR
7.2 nM
GARFT
65 nM
C110682卡铂98%41575-94-4100mg,250mg,1g,5g




P124220喷司他丁98%(HPLC)53910-25-15mg,25mg




F122998氟达拉滨98%21679-14-150mg,250mg,1g,5g




O124003奥沙利铂99%61825-94-325mg,100mg,500mg




C127663CX-5461≥98%1138549-36-65mg,25mg,100mgHCT-116细胞rRNA合成142 nM

A375细胞

MIA PaCa-2细胞

F1001495-氟尿嘧啶99%51-21-81g,5g,25g,100g,500g




C124969Capecitabine≥99%154361-50-9250mg,1g,5g,25g




F122999单磷酸氟达拉滨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细胞腺苷脱氨酶2.43 μM

U266, RPMI8226MM1.S细胞0.75 μM

U266, RPMI8226MM1.S细胞0.18 μM

R129835Raltitrexed≥98%112887-68-010mg,50mg,100mg




C102625克罗拉滨99%123318-82-15mg,20mg,25mg,100mg,500mg
Ribonucleotide reductase65 nM

I123381异环磷酰胺药用级3778-73-250mg,250mg,1g,5g




I123242异环磷酰胺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羟基脲98%127-07-11g,5g,25g,100g




F1107325-氟-2'-脱氧尿苷99%50-91-9100mg,250mg,500mg,1g,5g,25g




M1268586-巯基嘌呤 (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甲硝唑分析标准品,>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氮芥盐酸盐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维生素D298%50-14-61g,5g,25g
pol A123 mM

A1185591-(1-金刚烷基)乙基胺盐酸盐99%1501-84-41g,5g,25g,100g




M1118206-巯基嘌呤 一水合物98%6112-76-11g,5g,25g




M1118196-巯基嘌呤 一水合物99.50%6112-76-11g,5g,25g




P101249补骨脂素98%66-97-725mg,100mg,500mg




P101248补骨脂素分析标准品,≥98%66-97-720mg




C103233盐酸环胞苷98%10212-25-61g,5g,25g




N1248377-硝基吲哚-2-羧酸≥97%(HPLC)6960-45-8250mg,1g,5g
APE1~3 μM

N159515盐酸尼莫司汀>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佛手苷内酯>98.0%(GC)484-20-850mg,250mg,1g,5g




M101152佛手苷内酯分析标准品,>98.0%(GC)484-20-820mg




M1584395-甲氧基黄酮>98.0%(GC)42079-78-7200mg,1g,2.5g,5g




O131612噁喹酸98%14698-29-45g,25g




O114347噁喹酸分析标准品14698-29-4250mg




C139195盐酸阿糖胞苷≥99%69-74-9250mg,1g,5g,25g




B139600灭瘟素 S 盐酸盐≥96%3513-03-910mg,25mg,100mg




C154015氯氨布西>98.0%305-03-350mg,200mg,1g,5g




T102749异氰尿酸三缩水甘油酯98%2451-62-925g,100g,250g,500g




F129839Flupirtine maleate≥99%75507-68-510mg,25mg,100mg,1g




P128017Pyridostatin-1085412-37-85mg,10mg,25mg,50mg,100mg无细胞G-quadruplexe
490 nM
B107423硫酸博来霉素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'-脱氧尿苷(BUdR)99%59-14-3250mg,1g,5g,25g




G104274鸟嘌呤99%73-40-55g,25g,100g,250g,500g




D1003632’-脱氧尿苷99%951-78-01g,5g,25g




A1295678-氮杂鸟嘌呤≥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'-三磷酸二钠盐(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’-三磷酸尿苷三钠(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%,用于细胞培养58-96-85g,25g




U108810尿嘧啶核苷99%58-96-85g,25g,100g




T108392胸腺嘧啶99%,用于细胞培养65-71-45g,25g




T108391胸腺嘧啶99%65-71-45g,25g,100g,500g




 

*Sirtuin

项目号产品名称规格CAS包装细胞靶点IC50EC50
E129892EX 527 (Selisistat)≥98%49843-98-35mg,10mg,50mg无细胞SIRT138 nM
N108087烟酰胺用于细胞和昆虫细胞培养,≥99.5% (HPLC)98-92-0100g,500g



N108086烟酰胺≥99.5%(HPLC)98-92-0100g,250g,500g



N105043烟酰胺分析标准品,≥99.8%98-92-01g



N105042烟酰胺99%98-92-0100g,500g



S129890SRT1720≥98%1001645-58-45mg,10mg,50mg无细胞SIRT1
0.16 μM
S140425丹酚酸 B分析标准品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槲皮素分析标准品,≥98.5%117-39-520mg
PI3Kδ3.0 μM
Q118458槲皮素,二水分析标准品,≥98%(HPLC)6151-25-320mg



Q104838槲皮素,二水97%6151-25-35g,10g,25g,50g,100g,250g,500g



 

*Topoisomerase

项目号产品名称规格CAS包装细胞靶点IC50Ki
D107159盐酸阿霉素98%25316-40-925mg,100mg,250mg,500mg,1g,5g
Topo II

E121713Etoposide98%33419-42-0100mg,250mg,500mg,1g,5g
Topo II 

C111282(S)-(+)-喜树碱97%7689-03-4100mg,250mg,1g,5g
Topo I 0.68 μM
C111281(S)-(+)-喜树碱分析标准品,≥98%7689-03-420mg
Topo I 0.68 μM
T294611盐酸拓扑替康98%119413-54-650mg,250mg无细胞Topo I (MCF-7 Luc细胞)13 nM
Topo I (DU-145 Luc细胞)2 nM
T103153盐酸拓扑替康分析标准品,≥99%(HPLC)119413-54-610mg,50mg无细胞Topo I (MCF-7 Luc细胞)13 nM
Topo I (DU-145 Luc细胞)2 nM
I129863Idarubicin HCl≥98%57852-57-01mg,5mg,10mg,50mg无细胞Topo II (MCF-7 cells) 3.3 ng/mL
R139432鲁比特康≥98.0%(HPLC)91421-42-025mg,100mg



E122334盐酸表柔比星≥98% (HPLC)56390-09-15mg,25mg



M129460Mitoxantrone dihydrochloride≥97%70476-82-310mg,50mg,250mg,1g



D122335盐酸佐柔比星>90%23541-50-610mg,50mg,250mg无细胞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羟基喜树碱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金雀异黄酮分析标准品,≥98%446-72-020mg,1g,5gNIH-3T3细胞EGFR12μM
topo II19 μM
G106673金雀异黄酮97%446-72-0100mg,500mg,1g,5g,25gNIH-3T3细胞EGFR12μM
topo II19 μM
L157745Levofloxacin>98.0%(HPLC)100986-85-45g,25g,100g,500g



P129867Pirarubicin≥97%72496-41-410mg,50mg
Topo II

M139937马波沙星98%115550-35-11g,5g,25g



M114260马波沙星分析标准品115550-35-1100mg



C129896Ciprofloxacin≥98%85721-33-15g,25g,100g



N129248Novobiocin Sodium≥95%1476-53-550mg,100mg,500mg,1g,5g



E194832依诺沙星98%74011-58-81g,5g,25g



O102014Ofloxacin98%82419-36-11g,5g,25g,100g



O102012Ofloxacin分析标准品,≥99.0%(HPLC)82419-36-1100mg



N114262诺氟沙星98%70458-96-71g,5g,25g,100g,500g



N114261诺氟沙星分析标准品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培氟沙星分析标准品149676-40-4100mg
Topo II

A107930盐酸胺苯吖啶≥98% (HPLC)54301-15-425mg,100mg



B129359Balofloxacin98%127294-70-6100mg,500mg



H1075365-硝基-8-羟基喹啉97%4008-48-45g,25g,100g



H196266(S)-10-羟基喜树碱98%19685-09-7500mg,1g,5g,25g



H109791(S)-10-羟基喜树碱分析标准品,98%19685-09-725mg,100mg



T166659Topotecan hydrochloride hydrate98% (HPLC and enzymatic)123948-87-810mg,20mg,50mg



B123958白桦脂酸97%472-15-1100mg,1g,5g



B101534白桦脂酸分析标准品,>98%472-15-120mg



E1348527-乙基喜树碱≥96.0%(HPLC)78287-27-150mg,250mg,1g,5g,25g



F131683氟甲喹≥98.0%42835-25-61g,5g,25g,100g



F114353氟甲喹分析标准品42835-25-6250mg
Topo II15 μM


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