细胞周期/DNA损伤相关高活性小分子抑制剂

时间: 2020-04-23
作者: 百灵威
分享:
细胞周期/DNA损伤相关高活性小分子抑制剂-百灵威

细胞周期包括DNA合成(S期)和有丝分裂(M期)两个阶段,S期和M期被间隔期G1期和G2期分隔(图1)。细胞周期可以被细胞内外的各种信号所调控,为确保周期内每一时相事件有序完成并与外界环境因素相联系,需要细胞周期检查点的调控,在此期间可以监测细胞生长和DNA完整性的蛋白质是必不可少的。异常的细胞分裂或受损 DNA 的传播会导致肿瘤的发生。

环境中物理或化学的污染因素均会引起机体内细胞DNA结构的改变,即DNA损伤,如果未能及时进行DNA损伤修复,就可能发生细胞衰老、细胞凋亡和细胞癌变。

百灵威提供细胞周期/DNA损伤信号通路中的小分子抑制剂,可作用于CDK、PLK、HDAC等多个肿瘤研究靶点:

  • 靶点清晰明确,便于选择;
  • >80%的产品纯度高于98%
  • 生物活性经多客户验证
  • 90%以上有现货;
  • 性价比高:同比每个产品可节约5%-20%成本。
图1 真核细胞细胞周期示意图 <sup>[1]</sup>
图1 真核细胞细胞周期示意图 [1]
产品列表(按靶点分类)
618339
667463-62-9
GSK 3 Inhibitor IX, 99%
Description:
a potent, selective, reversible and ATP-competitive inhibitor
2286674
199986-75-9
CVT-313, 98%
Description:
a potent, selective, reversible, and ATP-competitive inhibitor of CDK2
555545
142273-20-9
Kenpaullone, 98%
Description:
a potent inhibitor of CDK1/cyclin B and GSK-3β
144505
161058-83-9
NU2058, 99%
Description:
a guanine-based CDK inhibitor
338303
212844-53-6
Purvalanol A, 98%
Description:
a potent CDK inhibitor
100441
212844-54-7
Purvalanol B, 97%
Description:
a cyclin-dependent kinase inhibitor
2062938
872573-93-8
Ro-3306, 96%
Description:
a potent and selective inhibitor of CDK1
1004546
345627-80-7
SNS-032, 99%
Description:
a selective CDK2 inhibitor
1232528
443797-96-4
JNJ-7706621, 98%
Description:
a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2
804158
722544-51-6
Barasertib-HQPA, 98%
Description:
a highly selective Aurora B inhibitor
1563114
422513-13-1
Hesperadin, 98%
Description:
an ATP-competitive inhibitor of aurora B kinase
583852
656820-32-5
Reversine, 98%
Description:
a novel class of ATP-competitive Aurora kinase inhibitor
1750763
1228591-30-7
TAK-632, 98%
Description:
a potent pan-RAF inhibitor
1415853
398493-79-3
PHA-680632, 98%
Description:
an aurora kinase inhibitor
624601
516480-79-8
BML-277, 97%
Description:
a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM
790544
155558-32-0
Hydroxyfasudil hydrochloride, 98%
Description:
a ROCK inhibitor
1018947
1226056-71-8
Thiazovivin, 98%
Description:
a potent ROCK inhibitor, which can protect human embryonic stem cells
262595
146986-50-7
Y-27632, 99%
Description:
an ATP-competitive inhibitor of ROCK-I and ROCK-II
101990
105628-07-7
Fasudil hydrochloride, 98%
Description:
a nonspecific ROCK inhibitor , with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively
1417791
129830-38-2
Y-27632 dihydrochloride, 99%
Description:
a selective ROCK1 (p160ROCK) inhibitor
9016864
1342278-01-6
RKI-1447, 98%
Description:
a potent small molecule inhibitor of ROCK1 and ROCK2
1684267
1062243-51-9
Ro3280, 99%
Description:
a potent, highly selective inhibitor of PLK1
2286710
1052532-15-6
SBE13 Hydrochloride, 98%
Description:
a potent and selective Plk1 inhibitor
165146
1784-03-8
TAME hydrochloride, 99%
Description:
an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest
190614
446-86-6
Azathioprine, 98%
Description:
a drug that suppresses the immune system and is used in organ transplantation and autoimmune disease
2062986
910462-43-0
Domatinostat, 98%
Description:
a selective class I HDAC inhibitor
2275937
1375465-91-0
ACY-738, 99%
Description:
a potent, selective and orally-bioavailable HDAC6 inhibitor
1834845
1314890-29-3
TMP269, 98%
Description:
a novel and selective class Iia histone deacetylase (HDAC) inhibitor
1831353
1440209-96-0
BRD73954, 98%
Description:
a potent and selective HDAC inhibitor
1833694
1418033-25-6
LMK-235, 99%
Description:
a potent and selective HDAC4/5 inhibitor
1833307
1429651-50-2
HPOB, 95%
Description:
a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6)
1891183
1252003-15-8
Tubastatin-A, 98%
Description:
a potent and selective HDAC6 inhibitor
2286551
1477949-42-0
Santacruzamate A, 98%
Description:
a potent and selective HDAC2 inhibitor
926452
251456-60-7
M344, 98%
Description:
an inhibitor of histone deacetylase (IC50=100 nM)
2286670
937039-45-7
Pimelic Diphenylamide 106, 98%
Description:
a slow, tight-binding inhibitor
786110
848354-66-5
PTACH, 98%
Description:
a SAHA-based novel inhibitor of human HDAC
1811748
1357389-11-7
RGFP966, 98%
Description:
a highly selective HDAC3 inhibitor
836786
537034-15-4
NKL 22, 98%
Description:
a HDAC inhibitor
1834137
1403783-31-2
Nexturastat A, 98%
Description:
a potent and selective HDAC6 inhibitor
2286671
537672-41-6
UF010, 98%
Description:
a potent and selective HADC inhibitor
447634
287383-59-9
Scriptaid, 98%
Description:
a potent histone deacetylase (HDAC) inhibitor, used in cancer research
1004535
128517-07-7
Romidepsin, 98%
Description:
a potent HDAC1 and HDAC2 inhibitor
1564431
1310693-92-5
Tubastatin A HCl, 98%
Description:
a potent and selective HDAC6 inhibitor
1831227
926259-99-6
BG45, 98%
Description:
a HDAC class I inhibitor with selectivity for HDAC3
245478
1716-12-7
Sodium phenylbutyrate, 98%
Description:
a histone deacetylase inhibitor
1759204
1080622-86-1
CP-466722, 98%
Description:
a rapidly reversible inhibitor of ATM
1684910
1345675-02-6
ETP46464, 99%
Description:
an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 Nm respectively.
1564473
1232410-49-9
VE-821, 99%
Description:
a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
1564012
905973-89-9
CGK733, 98%
Description:
a potent ATM/ATR inhibitor
1239105
925701-49-1
KU-60019, 98%
Description:
an improved KU-55933 analog
2276005
1380672-07-0
G007-LK, 99%
Description:
a potent and selective inhibitor of TNKS1 and TNKS2
1018722
459868-92-9
Rucaparib phosphate, 98%
Description:
a potent and oral PARP inhibitor
1445468
664993-53-7
JW 55, 99%
Description:
a potent and selective β-catenin signaling pathway inhibitor
1833902
92831-11-3
MN-64, 98%
Description:
a potent tankyrase 1 inhibitor
1413167
283173-50-2
Rucaparib, 98%
Description:
an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay,
968129
344458-15-7
PJ34 Hydrochloride, 97%
Description:
an inhibitor of PARPl1/2 with IC50 of 110 nM and 86 nM, respectively.
161191
3544-24-9
3-Aminobenzamide, 98%
Description:
a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion
942871
763113-22-0
Olaparib, 99%
Description:
PARP inhibitor
2286544
1609960-30-6
TH287, 97%
Description:
a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM
1866853
1609960-31-7
TH588, 99%
Description:
a first-in-class nudix hydrolase family inhibitor
918053
103060-53-3
Daptomycin, 99%
Description:
a lipopeptide antibiotic
1888727
1533426-72-0
SCR7, 99%
Description:
a DNA Ligase IV inhibitor with anticancer activity
150210
18942-26-2
Chebulinic acid, 98%
Description:
a potent natural inhibitor of M. tuberculosis DNA gyrase
242090
73-24-5
Adenine, 100%
Description:
a purine derivative and a nucleobase with a variety of roles in biochemistry
258050
4291-63-8
2-Chloro-2'-deoxyadenosine, 99%
Description:
an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis
271269
122111-03-9
Gemcitabine hydrochloride, 99%
Description:
a DNA synthesis inhibitor with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells, respectively.
274238
443-48-1
Metronidazole, 99%
Description:
a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa
293018
127-07-1
Hydroxyurea, 98%
Description:
a cell apoptosis inducer that inhibit DNA synthesis through inhibition of ribonucleotide reductase
349577
10212-25-6
Cyclocytidine hydrochloride, 98%
Description:
an important antileukemia drugs
366272
147-94-4
Cytosine β-D-arabinofuranoside, 99%
Description:
an antimetabolic agent and DNA synthesis inhibitor
382010
321-30-2
Adenine sulfate, 99%
Description:
a purine derivative
391047
73-24-5
Adenine, 99%
Description:
a purine derivative and a nucleobase with a variety of roles in biochemistry
392078
154361-50-9
Capecitabine, 99%
Description:
an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase
399796
58-96-8
Uridine, 99%
Description:
a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond
405632
2922-28-3
Adenine hydrochloride, 98%
Description:
a purine derivative with a variety of roles in biochemistry
588536
13292-46-1
Rifampicin, 98%
Description:
a potent and broad spectrum antibiotic against bacterial pathogens
792435
103060-53-3
Daptomycin, 95%
Description:
a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms
904475
75507-68-5
Flupirtine maleate salt, 97%
Description:
a selective neuronal potassium channel opener, NMDA receptor antagonist
1563982
309271-94-1
Inauhzin, 98%
Description:
a dual SirT1/IMPDH2 inhibitor
125841
98-92-0
Nicotinamide, 98%
Description:
an inhibitor of SIRT1
259196
501-36-0
Resveratrol, 98%
Description:
a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties
1349110
372196-77-5
PIK-75, 99%
Description:
a DNA-PK and PI3K inhibitor
920259
503468-95-9
KU-57788, 98%
Description:
a potent and selective inhibitor of DNA-PK
9005517
168425-64-7
Compound 401, 98%
Description:
a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM)
984758
119413-54-6
Topotecan Hydrochloride, 98%
Description:
a Topoisomerase I inhibitor with potent antineoplastic activities
217292
186826-86-8
Moxifloxacin Hydrochloride, 98%
Description:
a synthetic fluoroquinolone antibiotic agent
130846
97682-44-5
Irinotecan, 99%
Description:
a water soluble topoisomerase I inhibitor
460858
519-23-3
Ellipticine, 98%
Description:
a potent antineoplastic agent; inhibits DNA topoisomerase II activities
2286646
522650-83-5
SW044248, 98%
Description:
a non-canonical topoisomerase I inhibitor
113424
25316-40-9
Doxorubicin hydrochloride, 98%
Description:
an antibiotic agent
114089
86639-52-3
SN-38, 99%
Description:
an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively
116557
23541-50-6
Daunorubicin hydrochloride, 97%
Description:
an inhibits both DNA and RNA synthesis
194237
56390-09-1
Epirubicin hydrochloride, 98%
Description:
a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibiting Topoisomerase
289285
70476-82-3
Mitoxantrone hydrochloride, 99%
Description:
a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM
320523
33419-42-0
Etoposide, 98%
Description:
a chemotherapy medication used for the treatments of a number of types of cancer, inhibits DNA synthesis by forming a complex with topoisomerase II and DNA
563738
29767-20-2
Teniposide, 98%
Description:
N/A
987783
136572-09-3
Irinotecan hydrochloride trihydrate, 98%
Description:
a water soluble topoisomerase I inhibitor with antitumor activity
921481
85622-93-1
Temozolomide, 99%
Description:
an oral DNA alkylating agent used to treat some brain cancers,Solubility:≥20.83 mg/mL (DMSO)
964150
52-24-4
Thio-TEPA, 98%
Description:
a DNA alkylating agent, with antitumor activity
251696
61825-94-3
Oxaliplatin, 95%
Description:
a DNA/RNA synthesis inhibitor
274584
41575-94-4
Carboplatin, 98%
Description:
a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death
275688
15663-27-1
cis-Diamineplatinum(II) dichloride, 99%
Description:
a DNA/RNA synthesis inhibitor
591713
3543-75-7
Bendamustine hydrochloride, 98%
Description:
a DNA-damaging agent
608272
3778-73-2
Ifosfamide, 98%
Description:
an alkylating chemotherapeutic agent with activity against a wide range of tumors
996989
21679-14-1
Fludarabine, 98%
Description:
a DNA synthesis inhibitor
925039
121032-29-9
Nelarabine, 98%
Description:
a purine nucleoside analog and DNA synthesis inhibitor
150037
320-67-2
5-Azacytidine, 99%
Description:
a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases
180939
51-21-8
5-Fluorouracil, 99%
Description:
a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools
241600
50-91-9
2'-Deoxy-5-fluorouridine, 98%
Description:
an oncology drug that belongs to the class known as antimetabolites with an GI50 of 5.1 μM for the inhibition of PEPT1
255294
5536-17-4
Vidarabine, 98%
Description:
an antiviral drug which is active against herpes simplex and varicella zoster viruses
308447
4342-03-4
Dacarbazine, 98%
Description:
an antineoplastic agent
330390
123318-82-1
Clofarabine, 98%
Description:
a ribonucleotide reductase inhibitor
339804
2353-33-5
5-Aza-2'-deoxycytidine, 99%
Description:
a potent inhibitor of DNA methyltransferase
409544
6112-76-1
6-Mercaptopurine monohydrate, 99%
Description:
a DNA/RNA synthesis inhibitor
515848
17902-23-7
Tegafur, 98%
Description:
a chemotherapeutic 5-FU prodrug used in the treatment of cancers; is a component of tegafur-uracil
552943
70-00-8
Trifluorothymidine, 98%
Description:
an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis
579031
59-14-3
5-Bromo-2'-deoxyuridine, 99%
Description:
a nucleoside analog that competes with thymidine for incorporation into DNA. 5-BrdU is commonly used in the detection of proliferating cells
2286522
1000998-59-3
BMS-687453, 99%
Description:
a potent and selective PPARα agonist
2128986
1014691-61-2
GSK-0660, 99%
Description:
a potent antagonist of PPARβ and PPARδ
1683162
188591-46-0
GSK3787, 96%
Description:
a irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist
2275949
1233948-35-0
ELR510444, 98%
Description:
a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation
618172
168555-66-6
Fosbretabulin disodium, 98%
Description:
a microtubule destabilizing drug, a type of vascular-targeting agent,Solubility:≥4.5 mg/mL (H2O)
890634
219989-84-1
Ixabepilone, 98%
Description:
an orally bioavailable microtubule inhibitor
1867993
1338247-30-5
BMS-3, 98%
Description:
a potent LIMK inhibitor
1867994
1338247-35-0
BMS-5, 98%
Description:
a potent LIMK inhibitor
998523
19542-67-7
BAY 11-7082, 99%
Description:
a NF-κB inhibitor
952639
1572414-83-5
ML-323, 99%
Description:
a reversible, potent USP1-UAF1 inhibitor
914942
882257-11-6
P005091, 99%
Description:
a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7)
977952
856243-80-6
WP1130, 99%
Description:
a cell-permeable deubiquitinase (DUB) inhibitor
268355
154-42-7
2-Amino-6-purinethiol, 98%
Description:
an anti-leukemia and immunosuppressant agent
913396
301836-43-1
D4476, 99%
Description:
a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1)
624971
186611-52-9
IC261, 99%
Description:
a selective, ATP-competitive CK1 inhibitor
1734614
639052-78-1
LH846, 98%
Description:
a selective inhibitor of CKIδ
1433443
950912-80-8
PF-670462, 98%
Description:
a potent and selective inhibitor of casein kinase (CK1ε and CK1δ)
1239125
1009820-21-6
Silmitasertib, 98%
Description:
a potent and selective ATP-competitive CK2 inhibitor
1831796
1594094-64-0
CW-069, 98%
Description:
an allosteric inhibitor of HSET
1998866
72926-24-0
K858 Racemic, 98%
Description:
an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM
804505
863774-58-7
Dimethylenastron, 98%
Description:
a potent Eg5 inhibitor, with an IC50 of 200 nM
1561729
312756-74-4
RS-1, 98%
Description:
a RAD51 activator
1761875
415713-60-9
RI-1, 99%
Description:
a RAD51 inhibitor with IC50 ranging from 5 to 30 μM
1417810
847559-80-2
VER-82576, 98%
Description:
a potent, orally available and selective Hsp90 inhibitor
525549
50924-49-7
Mizoribine, 98%
Description:
a DNA/RNA synthesis inhibitor
935721
150399-23-8
Pemetrexed disodium, 99%
Description:
a novel antifolate
1564220
307543-71-1
STF-083010, 98%
Description:
an Ire1 inhibitor
1868030
1246529-32-7
MPI-0479605, 99%
Description:
a potent and selective ATP-competitive inhibitor of Mps1
1761087
1124329-14-1
AZ3146, 98%
Description:
a reasonably potent and selective Mps1 inhibitor
994764
1418013-75-8
NMS-873, 98%
Description:
a potent, selective allosteric VCP/p97 inhibitor
2286509
1286739-19-2
FRAX597, 99%
Description:
a potent group I p21-activated Kinases (PAKs) inhibitor
2286695
1643913-93-2
KPT-9274, 98%
Description:
an orally bioavailable, dual PAK4/ Nampt inhibitor
1578772
1337531-36-8
GSK2606414, 99%
Description:
a cell-permeable and orally available PERK inhibitor
相关文章

  1. Robert J. Duronio, Yue Xiong. Signaling Pathways that Control Cell Proliferation. Cold Spring Harb Perspect Biol. 2013, 5(3), a008904.