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19

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9595 LP-261

Microtubule Associated Cytoskeletal Signaling
LP-261 是一种新型的微管蛋白靶向抗癌剂,可与微管蛋白上的秋水仙碱位点结合,诱导 G2/M 期阻滞,其EC50为 3.2 μM。它可抑制人非小细胞肺癌的生长,可用于癌症研究。
T8492 BO-264

Apoptosis; FGFR Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
BO-264 是一种有口服活性的转化酸性卷曲螺旋 3 抑制剂,可特异性阻断 FGFR3-TACC3融合蛋白的功能。它诱导纺锤体检查点依赖的有丝分裂阻滞,DNA 损伤和细胞凋亡,具有广谱抗肿瘤活性。
T3330L cis-trismethoxy Resveratrol

(Z)-3,5,4'-Trimethoxystilbene,顺式白藜芦醇三甲醚

Microtubule Associated Cytoskeletal Signaling
cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) 抑制微管蛋白聚合 (IC50 = 4 μM) 并具有抗有丝分裂作用。
T20506 Maleuric acid

N-Carbamoylmaleamic acid,AI3 32778,AI3-32778,AI332778

Others Others
Maleuric acid (N-Carbamoylmaleamic acid) 可抗有丝分裂,可与放射自显影技术结合起来用于生物研究。Maleuric acid 可用于改善动植物的生长和繁殖力以及治疗乳清酸缺乏症。
T34787 TAS-119

TAS119,TAS2104,TAS 2104,TAS-2104,TAS 119

Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
TAS-119 (TAS-2104) 是一种可口服且具有选择性和有效性的 Aurora A 抑制剂,IC50为1.0 nM。TAS-119 对 Aurora B 也具有抑制作用,IC50 为 95 nM。TAS-119 对 Aurora A 的亲和力比 Aurora B高。TAS-119 具有有效的抗肿瘤活性和潜在的抗有丝分裂活性。
T36674 DMU-212

Apoptosis; ERK Apoptosis; MAPK
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T10215 AAPK-25

Apoptosis; PLK; Aurora Kinase Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic
AAPK-25 是选择性的Aurora/PLK 激酶双重抑制剂,显示出抗肿瘤活性。它可造成有丝分裂延迟并阻滞前中期细胞,通过生物标志物组蛋白 H3Ser10磷酸化反应,导致细胞凋亡激增。
T40232 KIF18A-IN-1

KIF18A-IN-1

KIF18A-IN-1 is a potent inhibitor of the mitotic kinesin KIF18A. This compound demonstrates significant anti-tumor properties.
T13227 Tubulin inhibitor 1

Microtubule Associated Cytoskeletal Signaling
Tubulin inhibitor 1 is an inhibitor of tubulin, inhibits tubulin polymerization, with potent anti-tumor activity, induces cellular apoptosis causes and cellular mitotic arrest in the G2/M phase.
T18679 SC-VC-PAB-MMAE

Others Others
SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), comprising the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) connected through the cleavable linker SC-VC-PAB[1].
T39307 Azido-PEG4-Val-Cit-PAB-MMAE

Azido-PEG4-Val-Cit-PAB-MMAE

Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs), comprising the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor), connected through the cleavable linker Azido-PEG4-Val-Cit-PAB-OH.
T18736 SuO-Val-Cit-PAB-MMAE

Others Others
SuO-Val-Cit-PAB-MMAE is an ADC (antibody-drug conjugate) linker comprising the anti-mitotic monomethyl auristatin E (MMAE, a tubulin inhibitor) connected through the SuO-Val-Cit-PAB peptide.
T40596 Tasisulam sodium

LY 573636 sodium,Tasisulam sodium

Tasisulam is an anti-cancer compound that induces apoptosis through the intrinsic pathway, leading to the release of cytochrome c and caspase-dependent cell death. Additionally, tasisulam inhibits mitotic progression and triggers vascular normalization.
T78771 Tubulin inhibitor 36

Tubulin inhibitor 36 (Compound 10) 是新型高效微管蛋白抑制剂,可阻止微管蛋白聚合并诱发细胞凋亡,IC50值为1.5±0.1 μM。该化合物在抗有丝分裂中表现出显著活性,并对胶质母细胞瘤(GBM)细胞线有效,适用于胶质母细胞瘤(GBM)的抗肿瘤研究。
T62118 KIF18A-IN-4

KIF18A-IN-4 是一种中度有效的 ATP 和微管 (microtubule) 非竞争性 KIF18A 抑制剂,其 IC50 值为 6.16 μM。KIF18A-IN-4 能够选择性的作用于大量有丝分裂驱动蛋白和激酶,对微管蛋白组装无直接影响。KIF18A-IN-4 显示出抗肿瘤作用。
T68860 Iso-Fludelone

Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as we...
T68273 BNC105P

BNC105P is a benzofuran-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and antineoplastic activities. Upon administration vascular disrupting agent BNC105P, the disodium phosphate ester of BNC105, is rapidly converted to BNC105; in activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may result in a blockage of mitotic spindle formation, cell cycle arrest, and disruption of the tumor vasculature. Hypoxic conditions ensue, deprivi...
T68480 4SC-207

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T71082 DW532

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human ca...

化合物

LP-261
Cat.No: T9595
Synonym:
Target: Microtubule Associated
BO-264
Cat.No: T8492
Synonym:
Target: Apoptosis, FGFR
cis-trismethoxy Resveratrol
Cat.No: T3330L
Synonym: (Z)-3,5,4'-Trimethoxystilbene,顺式白藜芦醇三甲醚
Target: Microtubule Associated
Maleuric acid
Cat.No: T20506
Synonym: N-Carbamoylmaleamic acid,AI3 32778,AI3-32778,AI332778
Target: Others
TAS-119
Cat.No: T34787
Synonym: TAS119,TAS2104,TAS 2104,TAS-2104,TAS 119
Target: Aurora Kinase
DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
AAPK-25
Cat.No: T10215
Synonym:
Target: Apoptosis, PLK, Aurora Kinase
KIF18A-IN-1
Cat.No: T40232
Synonym: KIF18A-IN-1
Target:
Tubulin inhibitor 1
Cat.No: T13227
Synonym:
Target: Microtubule Associated
SC-VC-PAB-MMAE
Cat.No: T18679
Synonym:
Target: Others
Azido-PEG4-Val-Cit-PAB-MMAE
Cat.No: T39307
Synonym: Azido-PEG4-Val-Cit-PAB-MMAE
Target:
SuO-Val-Cit-PAB-MMAE
Cat.No: T18736
Synonym:
Target: Others
Tasisulam sodium
Cat.No: T40596
Synonym: LY 573636 sodium,Tasisulam sodium
Target:
Tubulin inhibitor 36
Cat.No: T78771
Synonym:
Target:
KIF18A-IN-4
Cat.No: T62118
Synonym:
Target:
Iso-Fludelone
Cat.No: T68860
Synonym:
Target:
BNC105P
Cat.No: T68273
Synonym:
Target:
4SC-207
Cat.No: T68480
Synonym:
Target:
DW532
Cat.No: T71082
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6213 Vinorelbine ditartrate

Vinorelbine Tartrate,Nor-5'-anhydrovinblastine ditartrate,KW-2307,Navelbine tartrate,长春瑞滨酒石酸盐,酒石酸长春瑞滨

Microtubule Associated; Autophagy Autophagy; Cytoskeletal Signaling
Vinorelbine ditartrate (KW-2307)是一种抗有丝分裂剂,能够抑制 Hela 细胞的增殖,IC50值为 1.25 nM。
T0968 Paclitaxel

Taxol,紫杉醇,NSC 125973

Apoptosis; Microtubule Associated; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling
Paclitaxel (Taxol) 属于天然产物,是一种微管聚合物稳定剂。Paclitaxel 具有抗肿瘤活性;通过诱导有丝分裂停滞、细胞凋亡、细胞自噬等,导致细胞死亡。
T6718 Zingerone

Gingerone,Vanillylacetone,姜酮,NSC 15335

NF-κB NF-κB
Zingerone (Vanillylacetone) 是一种从生姜中得到的无毒的甲氧基苯酚,具有抗炎、抗糖尿病、抗脂质过敏、抗腹泻、抗痉挛和抗肿瘤等活性。它作为抗有丝分裂剂,能够抑制神经母细胞瘤的生长。它能够缓解氧化应激和炎症,下调 NF-κB 介导的信号通路。
TQ0112 Tubulysin A

TubA

Microtubule Associated Cytoskeletal Signaling
Tubulysin A is a natural product from myxobacterial. It has many function in vitro assays, including anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, and anti-angiogenic.

天然产物

Vinorelbine ditartrate
Cat.No: T6213
Synonym: Vinorelbine Tartrate,Nor-5'-anhydrovinblastine ditartrate,KW-2307,Navelbine tartrate,长春瑞滨酒石酸盐,酒石酸长春瑞滨
Target: Microtubule Associated, Autophagy
Paclitaxel
Cat.No: T0968
Synonym: Taxol,紫杉醇,NSC 125973
Target: Apoptosis, Microtubule Associated, Autophagy
Zingerone
Cat.No: T6718
Synonym: Gingerone,Vanillylacetone,姜酮,NSC 15335
Target: NF-κB
Tubulysin A
Cat.No: TQ0112
Synonym: TubA
Target: Microtubule Associated
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