49
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3434 |
BAY1217389
|
Kinesin | Cytoskeletal Signaling |
BAY1217389 是一种有效的选择性单极纺锤体 1 (MPS1) 激酶抑制剂 ,IC50值小于10 nM。 | |||
T16130 |
Mps1-IN-3
|
Kinesin | Cytoskeletal Signaling |
Mps1-IN-3 是一种有效的选择性 MPS1 激酶抑制剂,IC50值为 50 nM。 | |||
T1839 |
Mps1-IN-2
|
Kinesin; PLK | Cell Cycle/Checkpoint; Cytoskeletal Signaling |
Mps1-IN-2 是一种 ATP 竞争性Mps1/Plk1选择性双重抑制剂,对 Mps1 的IC50和Kd 值分别为 145 和 12 nM,对 Plk1 的Kd 值为 61 nM。 | |||
T2689 |
AZ3146
AZ 3146 |
Kinesin | Cytoskeletal Signaling |
AZ3146 是一种选择性 Mps1 抑制剂,IC50为 35 nM。 | |||
T2313 |
MPI-0479605
|
Apoptosis; Kinesin | Apoptosis; Cytoskeletal Signaling |
MPI0479605 是一种选择性的,ATP 竞争性的 Mps1抑制剂,IC50值为 1.8 nM。 | |||
T12237 |
NMS-P715
|
Casein Kinase; Kinesin; MELK; MAPK | Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
NMS-P715 是一种 ATP 竞争性MPS1选择性抑制剂,IC50值为 182 nM。 | |||
T8487 |
Empesertib
BAY 1161909 |
Kinesin | Cytoskeletal Signaling |
Empesertib (BAY 1161909) 是一种口服有效的Mps1抑制剂,IC50值小于1 nM,具有潜在的抗肿瘤活性。 | |||
T14765 |
BOS-172722
|
Kinesin | Cytoskeletal Signaling |
BOS-172722 是一种单极纺锤体 1 (MPS1) 检查点抑制剂,对MPS1 (1 mM ATP) 和P-MPS1 的IC50值分别为 11 nM 和 63 nM。它可研究多种乳腺癌。 | |||
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。 | |||
T2241 |
Alisertib
MLN 8237,4-[[9-氯-7-(2-氟-6-甲氧基苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]-2-甲氧基苯甲酸 |
Apoptosis; Aurora Kinase; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Alisertib (MLN 8237) 是一种口服活性和选择性的Aurora A 激酶抑制剂,IC50值为 1.2 nM。它通过靶向白血病细胞中的AKT/mTOR/AMPK/p38途径诱导其凋亡和自噬,具有抗肿瘤活性。 | |||
T2255 |
SB-743921 hydrochloride
SB743921 HCl,SB743921 |
Kinesin; KSP | Cell Cycle/Checkpoint; Cytoskeletal Signaling |
SB-743921 hydrochloride (SB743921 HCl) 是一种有效的驱动蛋白纺锤体蛋白 KSP 抑制剂,Ki 值为 0.1 nM。 | |||
T9682 |
AZD-4877
AZD4877 |
Apoptosis; Kinesin | Apoptosis; Cytoskeletal Signaling |
AZD-4877 是一种高效的纺锤体驱动蛋白 (Eg5) 抑制剂,对其 IC50 值为 2 nM。 AZD-4877 是 Ispinesib 的另一种构型, 能够抑制细胞有丝分裂,诱导形成单极纺锤体表型,介导细胞凋亡(Apoptosis)。 AZD-4877 具有抗肿瘤活性,对循环外周血单核细胞 (PBMC)有抑制作用。 | |||
T9831 |
MKC-1
Ro-31-7453 |
Apoptosis; Akt; Microtubule Associated; mTOR | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MKC-1 (Ro-31-7453) 是一种口服生物可利用的小分子双吲哚基马来酰亚胺细胞周期抑制剂,具有潜在的抗肿瘤活性。 | |||
T5699 |
SSE15206
|
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
SSE15206 是一种克服多药耐药性的微管聚合抑制剂,其在 HCT116 细胞中的 GI50值为 197 nM。由于癌细胞中纺锤体形成不完整,导致 G2/M 停滞,有丝分裂异常。 | |||
T2103 |
Ispinesib
伊匹尼塞,伊斯平斯,CK0238273,SB-715992 |
Apoptosis; Kinesin; KSP | Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling |
Ispinesib (SB-715992) 是一种选择性可逆的驱动蛋白纺锤体蛋白抑制剂,具有抗肿瘤特性。 | |||
TQ0318 |
Filanesib
ARRY-520,ARRY 520 |
KSP | Cell Cycle/Checkpoint |
Filanesib (ARRY 520) 是一种选择性的驱动蛋白纺锤体蛋白(KSP)的抑制剂(IC50 = 6 nM),具有强大的抗增殖活性。 | |||
TQ0318L |
ARRY 520 hydrochloride
|
KSP | Cell Cycle/Checkpoint |
ARRY 520 hydrochloride 是一种驱动蛋白纺锤体蛋白 (KSP) 抑制剂。它通过凋亡诱导细胞死亡,并具有有效的抗增殖活性。 | |||
T2090 |
Lexibulin
CYT-997 |
Apoptosis; Reactive Oxygen Species; Microtubule Associated | Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB |
Lexibulin (CYT-997) 是一种微管蛋白聚集强效抑制剂,可诱导细胞凋亡,并诱导 GC 细胞中的线粒体ROS 生成。它对多种癌细胞的 IC50 值为 10-100n M,在体内外具有高细胞毒性和血管增生阻断作用。 | |||
T2511 |
Plinabulin
普那布林,NPI-2358 |
Microtubule Associated | Cytoskeletal Signaling |
Plinabulin (NPI-2358) 是一种抗微管蛋白解聚肿瘤细胞的血管破坏剂,选择性地靶向并结合到微管蛋白的秋水仙碱结合位点,从而中断微管动力学的平衡。它对人肿瘤细胞系具有抑制作用,对 HT-29 细胞系的IC50值为 9.8 nM。 | |||
T36816 |
S-trityl-L-Cysteine
STLC |
Kinesin | Cytoskeletal Signaling |
S-Trityl-L-cysteine 是别构驱动蛋白Eg5的选择性抑制剂。rityl-L-cysteine 抑制基础 ATPase 活性的IC50为 1 μM,抑制微管激活的 ATPase 活性的IC50为 140 nM。S-Trityl-L-cysteine 显示出抗肿瘤活性。 | |||
T28694 |
SB-743921 free base
SB743921,SB-921,SB921,SB-743921,GSK-743921,GSK-921 |
||
SB-743921, a kinesin spindle protein (KSP) inhibitor, is used potentially for the treatment of non-Hodgkin's lymphoma (NHL). | |||
T23865 |
CCT-271850
MPS1-IN-77,MPS1IN77,CCT271850,CCT 271850,MPS1 IN 77 |
||
CCT-271850 is an inhibitor of the spindle checkpoint function of Monospindle 1. | |||
T21321 |
MK-0731
|
||
MK-0731, a synthetic small molecule with potential antineoplastic activity, selectively inhibits kinesin spindle protein (KSP), leading to the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase and apoptosis in | |||
T73229 |
Mps1-IN-4
|
||
Mps1-IN-4,一种针对Monopolar spindle 1 (Mps1)的选择性抑制剂,展现出抗增殖特性,适用于癌症领域的研究。 | |||
T25418 |
Filanesib TFA
Filanesib trifluoroacetic acid,ARRY-520 TFA,ARRY 520 TFA,ARRY520 TFA |
||
Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during | |||
T38710 |
JH295
|
||
JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism. | |||
T68743 |
AZD4877 HCl
|
||
AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neur... | |||
T37050 |
MPS1/TTK Inhibitor
MPS1/TTK Inhibitor |
||
MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegr... | |||
T14906 |
CCT251455
|
Kinesin | Cytoskeletal Signaling |
CCT251455 is an inhibitor of mitotic kinase monopolar spindle 1 (MPS1; IC50: 3 nM). | |||
T17007 |
TC-Mps1-12
|
Kinesin | Cytoskeletal Signaling |
TC-Mps1-12 is an effective and selective inhibitor of monopolar spindle 1 (IC50: 6.4 nM) . | |||
T71232 |
Alisertib sodium hydrate
|
||
Alisertib sodium hydrate is a salt of Alisertib --- an inhibitor of Aurora A kinase with potential antineoplastic activity. Alisertib binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. | |||
T10373 |
(R)-Filanesib
(R)-ARRY-520 |
Others | Others |
(R)-Filanesib is the R-enantiomer of ARRY-520. (R)-Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor (IC50: 6 nM). | |||
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... | |||
T72757 |
TTK inhibitor 3
|
||
TTK inhibitor 3 是一种有效的选择性TTK(一种必需的纺锤体组装检查点酶)抑制剂,其IC50值为 3.0 nM。 | |||
T73195 |
EAPB 02303
|
||
EAPB 02303 是一种微管破坏剂和抑制剂。EAPB 02303 诱导有丝分裂停止和纺锤体组装损伤。因此,EAPB 02303 诱导细胞凋亡 (apoptosis) 并表现出抗肿瘤活性。EAPB 02303 在较低浓度下也表现出与紫杉醇 的强协同作用。 | |||
T73483 | RMS-07 | ||
RMS-07 是 Monopolar Spindle Kinase 1 (MPS1/TTK)的共价抑制剂,其 IC50值为 13.1 nM。RMS-07靶向激酶结构域的半胱氨酸。 | |||
T25025 | ALB-109564 dihydrochloride | ||
ALB-109564 dihydrochloride 是长春碱生物碱的半合成衍生物,是一种微管蛋白抑制剂和抗肿瘤药物。它与微管蛋白单体结合并抑制微管的形成,导致有丝分裂纺锤体组装的破坏和肿瘤细胞停滞在细胞周期的G2/M 期。 | |||
T37063 | Laulimalide | ||
Microtubule stabilizing agent. Potent inhibitor of cellular proliferation in cancer cell lines (IC50 reported to be 3-30 nM, dependent on cell line used). Causes cells to arrest in the prometaphase of the cell cycle, prevents formation of bipolar spindle and increases kinetochore tension in preformed spindles. Pryor et al (2002) The microtubule stabilizing agent laulimalide does not bind in the taxoid site, kills cells resistant to PacT. and epothilones, and may not require its epoxide moiety fo... | |||
T61061 | JH295 hydrate | ||
JH295 hydrate 通过 Cys22 烷基化从而抑制细胞Nek2,它是有效的,不可逆和选择性的NIMA 相关激酶 2 (Nek2)抑制剂 (IC50 = 770 nM)。JH295 hydrate 对有丝分裂激酶 Cdk1,Aurora B 或 Plk1 不具有活性,不干扰双极纺锤体组件或纺锤体组件检查点。 | |||
T68686 |
DAP-81
|
||
DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations. | |||
T70095 |
Mps1-IN-1 dihydrochloride
|
||
Mps1-IN-1 dihydrochloride 是一种有效的,ATP 竞争性 Mps1激酶抑制剂,IC50为 367 nM。Mps1-IN-1 dihydrochloride 抑制 Mps1有丝分裂激酶活性并沉默纺锤体组装检查点 (SAC) 功能。Mps1-IN-1 dihydrochloride 降低癌细胞和“正常”细胞的活力。 | |||
T68428 |
ZK-Thiazolidinone
|
||
ZK-Thiazolidinone, also known as TAL, is an ATP-competitive inhibitor of PLK1. In vitro, ZK-Thiazolidinone counteracts the role of Plk1 in previously established functions, notably, sister chromatid separation, centrosome maturation, and bipolar spindle assembly. In vivo, ZK-Thiazolidinone selectively inhibits PLK1 and causes a prometaphase-like mitotic (G2–M) arrest. ZK-Thiazolidinone inhibits human PLK1 (IC50, 19± 12 nM) and various human and mouse tumor cell lines (IC50, 0.2–1.3 μM). ZK-Thiaz... | |||
T71556 |
MK-1496
|
||
MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n... | |||
T78138 | SIC5-6 | Others | Others |
SIC5-6为一强效Separase抑制剂,此酶为大型半胱氨酸蛋白酶,关键参与有丝分裂与减数分裂中染色体分离,DNA损伤修复,中心体分离与复制,以及纺锤体稳定与伸长。Separase在众多实体瘤高表达,成为潜在的化疗靶标。 | |||
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... | |||
T38428 |
Alisertib sodium
MLN 8237 sodium |
||
Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity. | |||
T78125 |
PVZB1194
|
Kinesin | Cytoskeletal Signaling |
PVZB1194是一种联苯型激酶Eg5(亦称KIF11)抑制剂,与细胞周期相关,可以通过抑制Eg5的ATP酶活性导致细胞周期阻滞和细胞凋亡,从而显现抗癌潜力。该化合物与α4/α6变抗袋结合,展现ATP竞争性活性。 | |||
T62148 |
NW 1028
|
||
NW 1028 是一种 VCP/p97 的有效抑制剂。NW 1028 能够选择性作用于 p97 的 ND1L 结构域,抑制依赖于 p97 的报告基因的降解。NW 1028 能够良好的结合 ND1L (Kd: 100 nM) 和全长 p97 (Kd: 285 nM)。NW 1028 对细胞有丝分裂纺锤体具有调节作用。 | |||
T36199 |
AZD 1152 (hydrochloride)
|
||
AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of p... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN7041 |
(-)-Epipodophyllotoxin
|
Apoptosis | Apoptosis |
(-)-Epipodophyllotoxin 是一种从八角莲中分离的癌细胞抗增殖剂,在 HeLa 细胞和 MCF-7 细胞中的GI50值分别为 0.36 和 0.24 μM。它可在体外抑制有丝分裂纺锤体组装。 | |||
T1270 |
Vincristine sulfate
Leurocristine,22-Oxovincaleukoblastine sulfate,Leurocristine sulfate,硫酸长春新碱 |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Vincristine sulfate (Leurocristine sulfate) 是一种抗肿瘤长春花生物碱。在细胞周期的 S 期不可逆地与微管(Ki: 85 nM) 和纺锤体蛋白结合,并干扰有丝分裂纺锤体的形成。 | |||
T0190 |
Vinorelbine
长春瑞宾,KW-2307 base |
Microtubule Associated | Cytoskeletal Signaling |
Vinorelbine (KW-2307 base) 是一种半合成的长春花生物碱。它与微管蛋白结合并阻止有丝分裂纺锤体的形成,导致中期肿瘤细胞生长停滞。 | |||
T22455 |
Vindesine sulfate
DVA,Desacetylvinblastine amide,硫酸长春地辛,DAVA,Desacetyl Vinblastine amide,VDS |
Others | Others |
Vindesine sulfate (Desacetyl Vinblastine amide) 是一种长春花生物碱,它是长春碱的合成衍生物,与有丝分裂纺锤体的微管蛋白结合,导致微管结晶和有丝分裂停滞或细胞死亡。 | |||
T1121 |
Podofilox
鬼臼毒素,Podophyllotoxin,(+)-Shikonin |
Microtubule Associated; Topoisomerase | Cytoskeletal Signaling; DNA Damage/DNA Repair |
Podofilox ((+)-Shikonin) 是从八角莲中分离的一种木脂素,是微管组装和 DNA 拓扑异构酶 II 抑制剂。它对皮肤和粘膜有很强的刺激性,具有角质溶解作用,可用于治疗疣和角化病,具有潜在的抗肿瘤特性。 | |||
T32055 |
Hemiasterlin
NSC 695242,NSC-695242,Milnamide B,NSC695242,(-)-Hemiasterlin |
||
Hemiasterlin is a cytotoxic peptide that acts by inducing mitotic arrest and abnormal spindle formation. |