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 [1]
产品列表(按靶点分类)
Description:
a potent, selective, reversible and ATP-competitive inhibitor
Description:
a potent, selective, reversible, and ATP-competitive inhibitor of CDK2
Description:
a potent inhibitor of CDK1/cyclin B and GSK-3β
Description:
a guanine-based CDK inhibitor
Description:
a potent CDK inhibitor
Description:
a cyclin-dependent kinase inhibitor
Description:
a potent and selective inhibitor of CDK1
Description:
a selective CDK2 inhibitor
Description:
a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2
Description:
a highly selective Aurora B inhibitor
Description:
an ATP-competitive inhibitor of aurora B kinase
Description:
a novel class of ATP-competitive Aurora kinase inhibitor
Description:
a potent pan-RAF inhibitor
Description:
an aurora kinase inhibitor
Description:
a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM
Hydroxyfasudil hydrochloride, 98%
Description:
a ROCK inhibitor
Description:
a potent ROCK inhibitor, which can protect human embryonic stem cells
Description:
an ATP-competitive inhibitor of ROCK-I and ROCK-II
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
Y-27632 dihydrochloride, 99%
Description:
a selective ROCK1 (p160ROCK) inhibitor
Description:
a potent small molecule inhibitor of ROCK1 and ROCK2
Description:
a potent, highly selective inhibitor of PLK1
Description:
a potent and selective Plk1 inhibitor
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
Description:
a drug that suppresses the immune system and is used in organ transplantation and autoimmune disease
Description:
a selective class I HDAC inhibitor
Description:
a potent, selective and orally-bioavailable HDAC6 inhibitor
Description:
a novel and selective class Iia histone deacetylase (HDAC) inhibitor
Description:
a potent and selective HDAC inhibitor
Description:
a potent and selective HDAC4/5 inhibitor
Description:
a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6)
Description:
a potent and selective HDAC6 inhibitor
Description:
a potent and selective HDAC2 inhibitor
Description:
an inhibitor of histone deacetylase (IC50=100 nM)
Pimelic Diphenylamide 106, 98%
Description:
a slow, tight-binding inhibitor
Description:
a SAHA-based novel inhibitor of human HDAC
Description:
a highly selective HDAC3 inhibitor
Description:
a HDAC inhibitor
Description:
a potent and selective HDAC6 inhibitor
Description:
a potent and selective HADC inhibitor
Description:
a potent histone deacetylase (HDAC) inhibitor, used in cancer research
Description:
a potent HDAC1 and HDAC2 inhibitor
Description:
a potent and selective HDAC6 inhibitor
Description:
a HDAC class I inhibitor with selectivity for HDAC3
Sodium phenylbutyrate, 98%
Description:
a histone deacetylase inhibitor
Description:
a rapidly reversible inhibitor of ATM
Description:
an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 Nm respectively.
Description:
a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
Description:
a potent ATM/ATR inhibitor
Description:
an improved KU-55933 analog
Description:
a potent and selective inhibitor of TNKS1 and TNKS2
Description:
a potent and oral PARP inhibitor
Description:
a potent and selective β-catenin signaling pathway inhibitor
Description:
a potent tankyrase 1 inhibitor
Description:
an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay,
Description:
an inhibitor of PARPl1/2 with IC50 of 110 nM and 86 nM, respectively.
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
Description:
PARP inhibitor
Description:
a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM
Description:
a first-in-class nudix hydrolase family inhibitor
Description:
a lipopeptide antibiotic
Description:
a DNA Ligase IV inhibitor with anticancer activity
Description:
a potent natural inhibitor of M. tuberculosis DNA gyrase
Description:
a purine derivative and a nucleobase with a variety of roles in biochemistry
2-Chloro-2'-deoxyadenosine, 99%
Description:
an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis
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.
Description:
a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa
Description:
a cell apoptosis inducer that inhibit DNA synthesis through inhibition of ribonucleotide reductase
Cyclocytidine hydrochloride, 98%
Description:
an important antileukemia drugs
Cytosine β-D-arabinofuranoside, 99%
Description:
an antimetabolic agent and DNA synthesis inhibitor
Description:
a purine derivative
Description:
a purine derivative and a nucleobase with a variety of roles in biochemistry
Description:
an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase
Description:
a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond
Adenine hydrochloride, 98%
Description:
a purine derivative with a variety of roles in biochemistry
Description:
a potent and broad spectrum antibiotic against bacterial pathogens
Description:
a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms
Flupirtine maleate salt, 97%
Description:
a selective neuronal potassium channel opener, NMDA receptor antagonist
Description:
a dual SirT1/IMPDH2 inhibitor
Description:
an inhibitor of SIRT1
Description:
a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties
Description:
a DNA-PK and PI3K inhibitor
Description:
a potent and selective inhibitor of DNA-PK
Description:
a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM)
Topotecan Hydrochloride, 98%
Description:
a Topoisomerase I inhibitor with potent antineoplastic activities
Moxifloxacin Hydrochloride, 98%
Description:
a synthetic fluoroquinolone antibiotic agent
Description:
a water soluble topoisomerase I inhibitor
Description:
a potent antineoplastic agent; inhibits DNA topoisomerase II activities
Description:
a non-canonical topoisomerase I inhibitor
Doxorubicin hydrochloride, 98%
Description:
an antibiotic agent
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
Daunorubicin hydrochloride, 97%
Description:
an inhibits both DNA and RNA synthesis
Epirubicin hydrochloride, 98%
Description:
a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibiting Topoisomerase
Mitoxantrone hydrochloride, 99%
Description:
a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM
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
Irinotecan hydrochloride trihydrate, 98%
Description:
a water soluble topoisomerase I inhibitor with antitumor activity
Description:
an oral DNA alkylating agent used to treat some brain cancers,Solubility:≥20.83 mg/mL (DMSO)
Description:
a DNA alkylating agent, with antitumor activity
Description:
a DNA/RNA synthesis inhibitor
Description:
a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death
cis-Diamineplatinum(II) dichloride, 99%
Description:
a DNA/RNA synthesis inhibitor
Bendamustine hydrochloride, 98%
Description:
a DNA-damaging agent
Description:
an alkylating chemotherapeutic agent with activity against a wide range of tumors
Description:
a DNA synthesis inhibitor
Description:
a purine nucleoside analog and DNA synthesis inhibitor
Description:
a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases
Description:
a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools
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
Description:
an antiviral drug which is active against herpes simplex and varicella zoster viruses
Description:
an antineoplastic agent
Description:
a ribonucleotide reductase inhibitor
5-Aza-2'-deoxycytidine, 99%
Description:
a potent inhibitor of DNA methyltransferase
6-Mercaptopurine monohydrate, 99%
Description:
a DNA/RNA synthesis inhibitor
Description:
a chemotherapeutic 5-FU prodrug used in the treatment of cancers; is a component of tegafur-uracil
Description:
an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis
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
Description:
a potent and selective PPARα agonist
Description:
a potent antagonist of PPARβ and PPARδ
Description:
a irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist
Description:
a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation
Fosbretabulin disodium, 98%
Description:
a microtubule destabilizing drug, a type of vascular-targeting agent,Solubility:≥4.5 mg/mL (H2O)
Description:
an orally bioavailable microtubule inhibitor
Description:
a potent LIMK inhibitor
Description:
a potent LIMK inhibitor
Description:
a NF-κB inhibitor
Description:
a reversible, potent USP1-UAF1 inhibitor
Description:
a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7)
Description:
a cell-permeable deubiquitinase (DUB) inhibitor
2-Amino-6-purinethiol, 98%
Description:
an anti-leukemia and immunosuppressant agent
Description:
a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1)
Description:
a selective, ATP-competitive CK1 inhibitor
Description:
a selective inhibitor of CKIδ
Description:
a potent and selective inhibitor of casein kinase (CK1ε and CK1δ)
Description:
a potent and selective ATP-competitive CK2 inhibitor
Description:
an allosteric inhibitor of HSET
Description:
an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM
Description:
a potent Eg5 inhibitor, with an IC50 of 200 nM
Description:
a RAD51 activator
Description:
a RAD51 inhibitor with IC50 ranging from 5 to 30 μM
Description:
a potent, orally available and selective Hsp90 inhibitor
Description:
a DNA/RNA synthesis inhibitor
Description:
a novel antifolate
Description:
an Ire1 inhibitor
Description:
a potent and selective ATP-competitive inhibitor of Mps1
Description:
a reasonably potent and selective Mps1 inhibitor
Description:
a potent, selective allosteric VCP/p97 inhibitor
Description:
a potent group I p21-activated Kinases (PAKs) inhibitor
Description:
an orally bioavailable, dual PAK4/ Nampt inhibitor
Description:
a cell-permeable and orally available PERK inhibitor
相关文章
- Robert J. Duronio, Yue Xiong. Signaling Pathways that Control Cell Proliferation. Cold Spring Harb Perspect Biol. 2013, 5(3), a008904.