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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9040 |
Aurora kinase inhibitor-2
IUN-70219,Aurora Kinase Inhibitor II |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora kinase inhibitor-2 (IUN-70219) 是一种可渗透细胞的苯胺喹唑啉,可抑制极光激酶的活性,对Aurora A 和Aurora B 的IC50分别为 390 nM 和 240 nM。 | |||
T6767 |
TCS7010
Aurora A Inhibitor I |
Apoptosis; Aurora Kinase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
TCS7010 (Aurora A Inhibitor I) 是一种选择性的 Aurora A 抑制剂,IC50值为 3.4 nM。 | |||
T21981 |
Phthalazinone pyrazole
|
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Phthalazinone pyrazole 是强效、选择性和口服生物可利用的 Aurora-A 激酶抑制剂,IC50值为 0.031 μM。它抑制人胚胎干细胞向肝细胞样细胞分化过程中的上皮间质转化。它还可阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。 | |||
T8537 |
Tripolin A
(3E)-3-[(2,5-二羟基苯基)亚甲基]-1,3-二氢-2H-吲哚-2-酮 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Tripolin A 是一种特异性的非 ATP 竞争性 Aurora A 激酶抑制剂,对Aurora A 和Aurora B 的IC50分别为1.5 μM 和7 μM。 | |||
T23426 |
TC-A 2317 hydrochloride
|
Others; Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Others |
TC-A 2317 hydrochloride 是 Aurora 激酶 A 的抑制剂,Ki 为 1.2 nM,而 Aurora 激酶 B 的 Ki 为 101 nM。 TC-A 2317 hydrochloride 显示出抗肿瘤活性。 | |||
T11638 |
Ilorasertib hydrochloride
ABT-348 hydrochloride |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1 nM, 7 nM, 120 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM). | |||
T5524 |
Aurora kinase inhibitor-3
Aurora Kinase Inhibitor III |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) 是一种有效的,选择性 Aurora A 激酶抑制剂,IC50为 42 nM。 | |||
TQ0059 |
Ilorasertib
ABT-348 |
VEGFR; FLT; c-RET; PDGFR; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂,可抑制 Aurora A、Aurora B 和Aurora C,IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1,IC50为7 nM、3 nM 和 32 nM。 | |||
T2509 |
Tozasertib
MK-0457,VX 680 |
Aurora Kinase; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Tozasertib (MK-0457) 是一种 Aurora A/B/C 激酶抑制剂,Ki 值分别为 0.6、18和4.6 nM。它显示出对 190 多种不同激酶的选择性。 | |||
T6068 |
MK-5108
VX-689,MK5108 |
Aurora Kinase; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
MK-5108 (VX-689) 是一种高效且特异性的 Aurora-A 激酶抑制剂,IC50 值为 0.064 nM。 | |||
T6126 |
JNJ-7706621
JNJ 7706621 |
Apoptosis; CDK; Aurora Kinase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
JNJ-7706621 是一种aurora kinase 抑制剂,有效抑制CDK1和CDK2,对CDK1,CDK2,aurora-A 和aurora-B 的IC50值分别为 9 nM,3 nM,11 nM 和 15 nM。 | |||
T2611 |
CCT 137690
CCT137690 |
Apoptosis; Aurora Kinase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic |
CCT 137690是一种有口服活性的极光激酶抑制剂,对极光激酶A、B 和C 的IC50值分别为15、25 和19 nM。 | |||
T50110 |
CD532
|
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
CD532 是一种高效的 Aurora A 激酶抑制剂,IC50 值为 45 nM。CD532 可阻断 Aurora A 激酶活性,驱动 MYCN 降解,可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于研究癌症。 | |||
T6315 |
MLN8054
|
Casein Kinase; PKA; Src; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
MLN8054是一种有口服活性的高选择性极光激酶抑制剂,IC50值为4 nM。 | |||
T1825 |
Reversine
|
Aurora Kinase; Adenosine Receptor; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; Neuroscience |
Reversine 是一种 ATP-竞争性 Aurora kinase 抑制剂,作用于Aurora A、Aurora B 和Aurora C,IC50分别为 400、500 和 400 nM。 | |||
T17267 |
XL228
|
IGF-1R; Bcr-Abl; Src; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
XL228 是一种多靶点酪氨酸激酶抑制剂,对 Bcr-Abl、Aurora A、IGF-1R、Src 和 Lyn 的 IC50 分别为 5、3.1、1.6、6.1和 2 nM。 | |||
T34888 |
TL12-186
TL12 186,TL12186 |
CDK; Ligand for E3 Ligase | Cell Cycle/Checkpoint; PROTAC |
TL12-186 是一种依赖于 Cereblon 的激酶降解剂,可降解 CDK,BTK,FLT3,Aurora 等激酶。TL12-186 对 CDK2/cyclin A 和 CDK9/cyclin T1 有抑制作用,IC50 分别为 73 和 55 nM。 | |||
T2358 |
ENMD-2076
|
Apoptosis; VEGFR; FGFR; FLT; c-RET; PDGFR; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
ENMD2076是一种多靶点激酶抑制剂,抑制Aurora A、Flt3、KDR/VEGFR2、Flt4/VEGFR3、FGFR1、FGFR2、Src、PDGFRα的IC50值分别为1.86、14、58.2、15.9、92.7、70.8、20.2 and 56.4 nM。 | |||
T2271 |
SBE13 Hydrochloride
SBE 13 hydrochloride,SBE 13 HCl |
Apoptosis; PLK; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint |
SBE13 Hydrochloride (SBE 13 HCl) 是一种选择性的Plk1抑制剂,IC50值为 0.2 nM,对 Plk2 的IC50>66 μM,Plk3的IC50值为875 nM。 | |||
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。 | |||
T22288 |
(1E)-CFI-400437 dihydrochloride
CFI-400437 dihydrochloride |
PLK | Cell Cycle/Checkpoint |
(1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) 是一种选择性和有效的 polo 样激酶 4 (PLK4) 抑制剂,IC50为 0.6 nM。它还抑制 Aurora A、 Aurora B、 KDR 和 FLT-3,IC50分别为 0.37、0.21、0.48 和 0.18 μM,具有抗增殖活性。 | |||
T4428 |
CCT241736
|
FLT; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
CCT241736 是一种口服生物可利用的双重 FLT3/Aurora 激酶抑制剂,还抑制临床相关的 FLT3 耐药突变体,包括 FLT3-ITD 和 FLT3。它是 CCT137690 的高级类似物,是治疗人类恶性肿瘤的临床前开发候选物。 | |||
T35328 |
H-1152 dihydrochloride
H-1152 2HCl,H-1152 dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
H-1152 dihydrochloride (H-1152 2HCl) 是 Rho 相关蛋白激酶 (ROCK) 的特异性抑制剂,IC50 为 12 nM,Ki 为 1.6 nM。 H-1152 dihydrochloride 抑制 PKA、PKC、PKG、Aurora A 和 CaMKII,IC50 值分别为 3.03 μM、5.68 μM、0.360 μM、0.745 μM 和 0.180 μM。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T63773 |
Aurora kinase inhibitor-8
|
||
Aurora kinase inhibitor-8 是 Aurora 激酶的高度选择性抑制剂。 | |||
T68234 | BI-831266 | ||
BI-831266 is a potent and selective Aurora kinase B inhibitor. | |||
T10412 |
Aurora inhibitor 1
|
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora inhibitor 1 is a potent Aurora inhibitor (IC50: ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase). | |||
T62789 |
Aurora kinase inhibitor-9
|
||
Aurora kinase inhibitor-9 (compound 9d) 是一种有效的 AURKA/B 双极光激酶抑制剂,作用于 Aurora A (IC50: 0.093 μM)、Aurora B (IC50: 0.09 μM)。Aurora kinase inhibitor-9 具有广谱抗增殖活性。 | |||
T60783 | Aurora/LIM kinase-IN-1 | ||
Aurora/LIM kinase-IN-1 (Compound F114) 是aurora 和lim 激酶的有效双重抑制剂。Aurora/LIM kinase-IN-1 可抑制胶质母细胞瘤的增殖和侵袭,可能用于胶质母细胞瘤和其他癌症相关的药物研发。Aurora 和 LIM 激酶是分别参与肿瘤细胞分裂和细胞运动的激酶。 | |||
T24753 |
SA-16
SA 16 |
||
SA-16 is a potent dual inhibitor of PDK1 and Aurora kinase. | |||
T62647 | Aurora A inhibitor 2 | ||
Aurora A inhibitor 2 (Compound 16h) 是一个 Aurora A kinase 的有效抑制剂 (IC50: 21.94 nM)。Aurora A inhibitor 2 能诱导 MDA-MB-231 细胞中的 caspase 依赖性凋亡。 | |||
T36801 |
Binucleine 2
|
||
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division ... | |||
T68740 |
NVP-TAC544
|
||
NVP-TAC544 is a novel focal adhesion kinase (FAK) inhibitor, potently blocking kinase activity of FAK along with Aurora A, activated Cdc42-associated kinase 1 (ACK1), Met, insulin receptor (IR), TrkA, and IGF-1R. | |||
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. | |||
T39718 | Tinengotinib | ||
Tinengotinib, a novel compound, acts as a potent modulator of protein kinases including Aurora kinase and VEGFR kinase. With its unique properties, Tinengotinib holds promise for investigating diseases marked by abnormalities in these kinases, particularly cancer-related conditions (WO2018108079A1). | |||
T74174 | JB170 | ||
JB170 是一种强效且高度特异性的PROTAC 介导的AURORA-A 降解剂 (DC50=28 nM),通过将 Alisertib 连接至Cereblon 配体 Thalidomide 而形成。JB170 优先结合 AURORA-A (EC50=193 nM) 而不是 AURORA-B (EC50=1.4µM)。JB170 介导的 S 期阻滞是由 AURORA-A 耗竭引起的。JB170 对 AURORA-A 激酶的非催化功能具有很好的抑制能力。 | |||
T36932 | CD532 hydrochloride | ||
CD532 hydrochloride is a potent inhibitor of Aurora A kinase, having an IC50 of 45 nM. It not only blocks the activity of Aurora A kinase but also facilitates the degradation of the protein MYCN. Furthermore, CD532 hydrochloride interacts directly with AURKA, inducing a significant conformational change. Its utility in cancer research has been demonstrated [1][2]. | |||
T72522 |
Aurora kinase-IN-1
|
||
Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达,并下调 G1-to-S 进行性细胞周期蛋白,导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis)。Aurora 激酶-IN-1 是化疗药物的先导化合物。 | |||
T73800 |
Retreversine
|
||
Retreversine 是 Reversine 的无活性阴性对照。Reversine 是一种 ATP-竞争性的Aurora kinase 抑制剂。 | |||
T68332 |
AKI-001
|
||
AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near s... | |||
T21298 |
SNS-314
SNS-314 free base,SNS314,SNS 314 |
||
SNS-314, a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity, selectively binds and inhibits AKs A and B, resulting in the inhibition of cell division and proliferation in tumor cells that overexpress AKs. | |||
T61527 |
GSK2646264
|
||
GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1]. | |||
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. | |||
T71279 |
BPR1K653
|
||
BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent ... | |||
T82931 | Aurora A inhibitor 3 | Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora A inhibitor3 (Compound 5h) 是一种抑制Aurora-A激酶活性的化合物,IC50为0.78 μM。该化合物同时对MCF-7和MDA-MB-231细胞线表现出细胞毒性,其GI50值分别为0.12 μM和0.63 μM。 | |||
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... | |||
T78753 | Aurora Kinases-IN-4 | Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora Kinases-IN-4(Compound 11c)是共价ATP竞争型aurora kinaseA抑制剂,具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著,其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌(TNBC)的相关研究。 | |||
T14925 |
Cenisertib
AS-703569,R-763 |
Akt; Bcr-Abl; STAT | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Cenisertib 是一种有效的 ATP 竞争性的多激酶抑制剂,对 Aurora-kinase-A/B,ABL1,AKT,STAT5, FLT3 的活性具有抑制作用,对FER 及其同源物的激酶也显示出抑制作用。Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长,也抑制异种移植模型中胰腺癌,乳腺癌,结肠癌,卵巢癌和肺癌以及白血病的肿瘤生长。 | |||
T69296 |
PHA-680626
|
||
PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM). | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN3834 |
Derrone
|
Antifection | Microbiology/Virology |
Derrone may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens. It is also a novel Aurora kinase inhibitor, it can significantly inhibit the formation and growth of MCF7 tumor spheroids. |