52
8
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T40247 |
Ethofumesate
|
Others | Others |
Ethofumesate 是一种手性除草剂。Ethofumesate 通过抑制有丝分裂减少光合作用和植物呼吸。 | |||
T8561 |
Apcin
|
APC | Cell Cycle/Checkpoint |
Apcin 是后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性的有效竞争性抑制剂,可通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。它占据 WD40 结构域侧面的 D-box 结合口袋,并可以延长有丝分裂。它通过阻断有丝分裂退出并通过共同添加 Ts-Arg-OMe 协同放大而起作用。 | |||
T7200 |
TAK-960
|
PLK | Cell Cycle/Checkpoint |
TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂,IC50为 0.8 nM,对 PLK2 和 PLK3 也有抑制作用,IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖,可治疗多种肿瘤异种移植。 | |||
T21654 |
1-Oleoyl lysophosphatidic acid sodium
1-Oleoyl lysophosphatidic acid sodium salt |
LPA Receptor | GPCR/G Protein |
1-Oleoyl lysophosphatidic acid sodium (1-Oleoyl lysophosphatidic acid sodium salt) salt 是 LPA1 和 LPA2 的内源性激动剂,可通过诱导 DNA 合成促进有丝分裂,参与正常和病理性情绪反应,如焦虑和抑郁。 | |||
TQ0317 |
R1530
R-1530,R 1530 |
VEGFR; FGFR; FLT; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
R1530 是一种多激酶抑制剂,具有抗肿瘤和抗血管生成活性。它是具有口服活性的有丝分裂/血管生成高效双重作用抑制剂, 抑制 VGFR2、FGFR1作用的 IC50分别为 10 nM 和 28 nM。 | |||
T19664 |
ON1231320
GBO-006 |
Apoptosis; PLK | Apoptosis; Cell Cycle/Checkpoint |
ON1231320 (GBO-006) 是一种高度特异性的 polo 样激酶 2 抑制剂,IC50为 0.31 µM。在有丝分裂 G2/M 期阻断肿瘤细胞周期进程,它可导致细胞凋亡。它是一种芳基磺酰基吡啶并嘧啶酮,具有抗肿瘤活性。 | |||
T1992 |
Mertansine
DM1,Maytansinoid DM1 |
Microtubule Associated | Cytoskeletal Signaling |
Mertansine (DM1) 是一种微管蛋白抑制剂,也是一种抗体可缀合的美登木素生物碱。它通过连接体连接到单克隆抗体上,形成抗体偶联药物。 | |||
T24398 |
Lenaldekar
LDK |
Akt; IGF-1R; S6 Kinase | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Lenaldekar (LDK) 抑制 T 细胞扩增和自身免疫性脑脊髓炎。 Lenaldekar 导致 PI3 激酶/AKT/mTOR 通路成员的去磷酸化并延迟有丝分裂晚期的敏感细胞。 | |||
T3643 |
HMN-176
|
PLK | Cell Cycle/Checkpoint |
HMN176 是一种二苯乙烯衍生物,可抑制有丝分裂,干扰 polo 样激酶-1 (PLK1) | |||
T22305 |
Dexrazoxane
右雷佐生,ICRF-187 |
Others | Others |
Dexrazoxane (ICRF-187) 是一种心脏保护剂。 | |||
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。 | |||
T9014 |
SKI-178
|
Apoptosis; S1P Receptor | Apoptosis; GPCR/G Protein |
SKI-178 是一种鞘氨醇激酶-1(SphK1)和 SphK2抑制剂,以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。 | |||
T26585 |
AK301
AK-301,AK 301 |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
AK301 是一种强效的管蛋白聚合选择性抑制剂,也是癌细胞对凋亡配体的有效增敏剂(EC50 < 200 nM)。AK301 可阻止有丝分裂的结肠癌细胞在停用化合物并解除阻止后很容易发生 p53 依赖性凋亡。 | |||
T3352 |
XL413
|
cholecystokinin; Casein Kinase; Pim; CDK | Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; JAK/STAT signaling; Metabolism; Stem Cells |
XL413 是一种口服生物可利用的细胞分裂周期 7 同源物 (CDC7) 激酶抑制剂,具有潜在的抗肿瘤活性,IC50值为 3.4 nM。它对 pMCM 的 EC50值为 118 nM,对 CK2 和 PIM1 的 IC50值分别为 215 和 42 nM。 | |||
T4057 |
Hoechst 33258 trihydrochloride
Hoechst 33258,Pibenzimol,Bisbenzimide,H 33258 trihydrochloride,bisBenzimide H 33258 trihydrochloride,HOE 33258 |
Parasite | Microbiology/Virology |
Hoechst 33258 trihydrochloride (Bisbenzimide) 是一种能够用于 DNA 染色的荧光染料。 | |||
T3567 |
SU 4942
|
Others | Others |
SU-4942 是酪氨酸激酶信号传导调节剂。SU-4942 对 VEGF 和内皮细胞生长因子 (ECGF) 诱导的内皮细胞有丝分裂具有抑制作用。 | |||
T29059 |
UMK57
UMK 57,UMK-57 |
Kinesin | Cytoskeletal Signaling |
UMK57 是一种CENP-Ei、MCAK 增强剂,选择性促进 k-MT 附着错误纠正以抑制染色体错误分离的小分子化合物,可以通过破坏有丝分裂过程中动粒微管 (k-MT) 附着的稳定性来提高染色体分离保守性。 | |||
T70407 |
cemadotin free base
LU103793 free base |
Microtubule Associated | Cytoskeletal Signaling |
Cemadotin free base(LU103793 free base) 是一种新型的抗限定性肽 ,是一种新型的抗有丝分裂肽 ,是Dolastatin 15的类似物 。Dolastatin 15是一种天然存在的细胞毒肽,可阻断有丝分裂并抑制微管(管蛋白),Ki 为1μM。Cemadotin 用于研究抗癌。 | |||
T7055 |
Bz-RS-ISer(3-Ph)-Ome
Methyl (2R,3S)-3-(benzoylamino)-2-hydroxy-3-phenylpropanoate |
Others; HIV Protease | Microbiology/Virology; Others; Proteases/Proteasome |
Bz-RS-ISer(3-Ph)-Ome (Methyl (2R,3S)-3-(benzoylamino)-2-hydroxy-3-phenylpropanoate) 是紫杉醇衍生物,在低细胞毒性下抑制 HSV 复制周期,阻断 Vero 细胞的有丝分裂,影响 M-MSV 诱导的肿瘤大小,并通过抑制 PHA 诱导的 T 淋巴细胞增殖而影响免疫应答。 | |||
T16987 |
TAO Kinase inhibitor 1
|
Others; MAPK | MAPK; Others |
TAO Kinase inhibitor 1 是一种ATP 竞争性的thousand-and-one amino acid kinases (TAOK)选择性抑制剂,对于 TAOK1 和 TAOK2 的IC50s 分别为 11 nM 和 15 nM。它能够延迟有丝分裂以及诱导有丝分裂细胞死亡。 | |||
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。 | |||
T9864 |
Debio-0123
WEE1-IN-5 |
Wee1 | Cell Cycle/Checkpoint |
Debio-0123 (WEE1-IN-5) 是一种口服有效且高度特异性的WEE1抑制剂,IC50值在低纳摩尔范围内。Debio-0123 抑制磷酸化 CDC2。Debio-0123 可增强卡铂在体内的抗肿瘤活性,而这两种药物单独使用都没有活性。 | |||
T35570 |
Chiauranib
CS2164,西奥罗尼 |
c-Fms; VEGFR; FLT; PDGFR; c-Kit; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
Chiauranib 是一种针对肿瘤血管生成的多靶点抑制剂,具有强大的抗癌作用。 Chiauranib 有效抑制血管生成相关激酶(VEGFR1、VEGFR2、VEGFR3、PDGFRα 和 c-Kit)、有丝分裂相关激酶 Aurora B 和慢性炎症相关激酶 CSF1R,IC50 值范围为 1-9 nM。 | |||
T27407 |
GDC0575 monohydrochloride
ARRY-575,GDC-0575,GDC 0575,ARRY575,GDC0575 |
Chk | Cell Cycle/Checkpoint |
GDC0575 monohydrochloride (ARRY575) 是一种有效的、选择性的细胞周期检查点激酶 1(Chk1) 抑制剂,IC50 为 1.2 nM。GDC0575 monohydrochloride (ARRY575) 特异性结合并抑制 Chk1;这可能导致肿瘤细胞在 S 期和 G2/M 期绕过 Chk1 依赖性细胞周期停滞,从而允许细胞在进入有丝分裂之前进行 DNA 修复。 | |||
T11859L |
Litronesib
KF-89617,LY-2523355 |
Kinesin | Cytoskeletal Signaling |
Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity. | |||
T17163 | Trifluralin | Others | Others |
Trifluralin is a commonly used pre-emergence herbicide. It inhibits root development by interrupting mitosis and thus can control weeds as they germinate. | |||
T24699 |
R1498
R-1498,R 1498 |
||
R1498 is an inhibitor of cyclin-dependent kinase 2. It also acts by targeting angiogenesis and mitosis pathways. It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment. | |||
T29205 |
Zarilamide
Zarilamid |
||
Zarilamide is inhibitor of the nuclear division in germinating zoospore cysts of Phytophthora capsici. Zarilamide destructs the microtubule cytoskeleton, resulting in a consequent inhibition of mitosis. | |||
T38644 |
Docetaxal
PNU-101383,10-Acetyl docetaxel |
||
Docetaxal, also known as 10-Acetyl docetaxel, is an analog of Docetaxel exhibiting potent anticancer properties. It acts as a microtubule disassembly inhibitor, effectively inhibiting mitosis. | |||
T63375 |
FT709
|
||
FT709 是选择性的USP9X 有效抑制剂 (IC50: 82 nM)。其中USP9X 与中心体功能、EGF 受体降解、有丝分裂期间的染色体排列、化学致敏和昼夜节律有关。 | |||
T18361 |
MMAE-SMCC
|
Others | Others |
MMAE-SMCC is a drug-linker conjugate designed for antibody-drug conjugates (ADC). It consists of MMAE, a potent inhibitor of mitosis and tubulin, and SMCC, a linker that facilitates the development of ADCs. | |||
T68611 | GW837016X | ||
GW837016X, also known as NEU-391, is a potent inhibitor of protozoan parasite proliferation. GW837016X extended life of treated mice by 50%, compared to untreated controls. At the cellular level, GW837016X inhibited mitosis and cytokinesis in T. brucei. | |||
T81696 |
NBI-961
|
||
NBI-961为高效NEK2抑制剂,能阻断蛋白酶体降解作用。该化合物在弥漫性大B细胞淋巴瘤(DLBCL)细胞中诱导G2/有丝分裂停滞及细胞凋亡(apoptosis)。 | |||
T28179 |
NMK-TD-100
NMK-TD 100,NMK-TD100 |
||
NMK-TD-100 is a microtubule modulating agent with anti-proliferative activity by disrupting microtubule functions through tubulin binding. NMK-TD-100 blocks mitosis and induces apoptosis in HeLa cells by binding to tubulin. Polymerization of tissue purifi | |||
T76458 |
P34cdc2 Kinase Fragment
|
||
P34cdc2 Kinase Fragment,与酵母有丝分裂中DNA复制的完整度相关,并能磷酸化丝裂原激活蛋白MAP2,进而调节爪蟾卵母细胞减数分裂中的微管聚合活性。 | |||
T36979 |
Histone H3 (21-44)-GK-biotin amide (trifluoroacetate salt)
Histone H3 (21-44)-GK-biotin amide (trifluoroacetate salt) |
||
Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.3 sequence and is biotinylated via a C-terminal GK linker. Unlike histone H3.1 and H3.2, the histone H3.3 variant contains a serine residue at position 31 that is phosphorylated during late prometaphase and metaphase of mitosis. Histone H3 (21-44) also contains lysine residues at positions 23, 27, and 36 that are subject to methylation and acetylation, all of whi... | |||
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。 | |||
T36358 |
Diminutol
|
||
Diminutol is a cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 μM), to destabilize microtubules and disrupt mitosis. At 50 μM, it directly affects tubulin polymerization in Xenopus egg extracts without interfering with the activity of Cdk1, DNA replication, or actin polymerization. | |||
T68363 |
OUN10989
|
||
OUN10989, an analogue compound of LP-261, is a Potent Antimitotic Agent. OUN10989 exhibited potent inhibition of mitosis at the G2/M stage. OUN10989 was first reported in J. Med. Chem 54(1), 179-200; 2011 (compound 7). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). | |||
T82221 |
Head activator neuropeptide
|
||
Head activator neuropeptide 是一种源自哺乳动物细胞系的神经元或神经内分泌的有丝分裂原,其通过与GPR37结合来进行信号传递并促进细胞分裂。 | |||
T71218 | AEZS-112 | ||
AEZS-112, also known as ZEN012, is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase ... | |||
T68232 |
Epofolate
|
||
Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and s... | |||
TP2292 |
survivin (baculoviral IAP repeat-containing protein 5) (21-28)
|
Others | Others |
Survivin (baculoviral inhibitor of apoptosis IAP repeat-containing protein-5) is a member of the IAP gene family, which has been implicated in both inhibitions of apoptosis and mitosis regulation1. Survivin is one of the most uniformly up-regulated genes | |||
T71207 |
(R)-(+)-Blebbistatin O-Benzoate
|
||
(R)-(+)-Blebbistatin O-Benzoate is a derivative of Blebbistatin. (R)-(+)-Blebbistatin is a 1-phenyl-2-pyrrolidinone derivative and a selective inhibitor of non-muscle myosin II. It blocks cell blebbing rapidly and reversibly and also disrupts directed cell migration and cytokinesis in vertebrate cell. (R)-(+)-Blebbistatin can also inhibit contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly. (R)-(+)-Blebbistatin is suitable as a negative control for (S)-(-)-... | |||
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。 | |||
T69003 |
E7974
|
||
E7974 is an analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. Check for active clinical trials or closed cli... | |||
T62417 |
MELK-8a
|
||
MELK-8a (NVS-MELK8a) 是一种高效的、选择性的母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂 (IC50: 2 nM)。MELK-8a 也能够抑制 Flt3 (ITD) (IC50: 0.18 μM)、Haspin (IC50: 0.19 μM)、PDGFRα (IC50: 0.42 μM)。其中 MELK 在调节癌细胞的细胞有丝分裂中具有重要作用。 | |||
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... | |||
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... | |||
T70235 |
Cemadotin hydrochloride
|
||
Cemadotin hydrochloride is the salt from of Cemadotin (free base), also known as, LU103793, a mitosis inhibitor potentially for the treatment of solid tumours. Cemadotin is also a synthetic derivative of Dolastatin 15, an antiproliferative compound which was isolated from the mollusk Dolabella auricularia. Like Dolastatin 15, LU103793 is highly cytotoxic in vitro (IC50 = 0.1 nM). LU103793 inhibits microtubule polymerization in a concentration-dependent manner (IC50 = 7 microM). Treatment with ... |
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。 | |||
T0186 |
Docetaxel trihydrate
RP-56976 (Trihydrate),RP56976 (NSC 628503) Trihydrate,多西他赛三水合物 |
Apoptosis; BCL; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Docetaxel trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂,抑制微管解聚的IC50值为 0.2 μM。它是紫杉醇的半合成类似物,能减弱 bcl-2 和 bcl-xL 基因表达的影响。它阻滞G2/M 细胞周期,导致细胞凋亡。 | |||
T3S0209 |
Vincristine
|
ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR | Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling |
Vincristine 与微管蛋白结合并抑制微管的形成,从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂,用于研究治疗血液系统癌症,如白血病和淋巴瘤以及儿童肉瘤的相关研究。 | |||
TN4944 | Santamarine | Caspase | Apoptosis; Proteases/Proteasome |
Santamarine has significant anticancer activity, can inhibit L1210 cells because of its cytotoxic,cytostatic and blocking mitosis and reducing uptake of thymidine. Santamarine and reynosin show bactericidal activity against clinical strains of Mycobacterium tuberculosis. | |||
TN3724 |
Cryptomoscatone D2
|
p53 | Apoptosis |
Cryptomoscatone D2 is a highly efficacious inhibitor of the G(2) checkpoint, and G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis. | |||
T82787 |
Calythropsin
|
||
Calythropsin是一种对有丝分裂产生微弱影响的细胞毒性查尔酮类化合物,该化合物可能还会影响微管蛋白的聚合。 | |||
TN3721 |
Cryptofolione
|
Antifection | Microbiology/Virology |
Z-Cryptofolione and Cryptomoscatone D2 as highly efficacious inhibitors of the G(2) checkpoint, G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis. Cryptofolione shows moderate cytotoxicity in both macrophages and T. cruzi amastigotes, it also displays a mild inhibitory effect on the promastigote form of Leishmania spp. | |||
T75521 | PM050489 | ||
PM050489 是一种有效的聚酮类微管/微管蛋白 (Microtubule/Tubulin) 抑制剂,可从马达加斯加海绵Lithoplocamia lithistoides 中分离。PM050489 抑制有丝分裂,IC50值为 26.4 nM。PM050489 具有抗肿瘤活性,能用于癌症研究。 |