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29

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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).
T12010 Aurora B inhibitor 1

Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
Aurora B inhibitor 1 是一种 Aurora B (Aurora-1) 抑制剂(Ki <0.010 uM),具有潜在的抗癌活性,可用于研究癌症。
T63436 Aurora A inhibitor 1

Aurora A inhibitor 1 是有效的、选择性的 Aurora A 抑制剂。 Aurora A 与多种组织学起源的癌症有关,而且在过度表达时可能表现出致癌活性。Aurora A inhibitor 1 表现出潜力进行 Aurora A 介导的癌症疾病的研究。
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。
T6435 CCT129202

2-[4-[6-氯-2-(4-二甲基氨基苯基)-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]-N-(噻唑-2-基)乙酰胺

Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
CCT129202 是一种 ATP 竞争性泛极光激酶抑制剂,作用于 Aurora A、Aurora B 和 Aurora C,IC50 分别为 0.042 μM、0.198 μM 和 0.227 μM。
T6028 PF 477736

PF 00477736,PF-477736,PF-736,PF-00477736,PF477736

c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂,Ki 值为0.49 nM。它也是Chk2抑制剂,Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。
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。
T6380 AMG 900

AMG900,AMG-900,莪术醇.姜黄醇

p38 MAPK; Tyrosine Kinases; Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors
AMG 900 是一种有效且高度选择性的泛极光激酶抑制剂,对Aurora A、B 和C 的IC50分别为 5 nM、4 nM 和 1 nM。
T3068 AT9283

J-504568

Apoptosis; FLT; JAK; Bcr-Abl; Aurora Kinase; Autophagy Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
AT9283 (J-504568) 是一种多靶点激酶抑制剂,抑制多种实体瘤在体内外的生长和存活,有效抑制Aurora A/B,JAK2/3,Abl (T315I),和Flt3,IC50值范围为 1-30 nM。
T6129 GSK-1070916

GSK-1070916A,GSK1070916

Apoptosis; Tie-2; FLT; AMPK; Aurora Kinase Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
GSK-1070916 (GSK-1070916A) 是一种选择性,ATP 竞争型的极光激酶B/C 抑制剂,Ki 值分别为0.38和1.5 nM。
T6458 CYC-116

噻氯匹定

VEGFR; FLT; CDK; S6 Kinase; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
CYC116是一种有效的极光激酶 A 和 B 的抑制剂,Ki 值分别为8和9 nM。
T6039 TAK-285

TAK285,TAK 285

EGFR; MEK; HER; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors
TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂,IC50 分别为 17 和 23 nM。它可穿过血脑屏障,有抗肿瘤活性,对 HER1/2 的选择性是 HER4 的 10 倍以上。
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。
T71169 XMD-12

XMD-12, also known as DUN57447, Aurora inhibitor (compound 1) or Aurora-IN-1, is an Auroro inhibitor, which targets Aurora A/B/C. (5.6/18.4/24.6 nM).
T62945 Aurora A/PKC-IN-1

Aurora A/PKC-IN-1 (Compound 2e) 是一种有效的 Aurora A (AurA) 和 PKC (α, β1, β2, θ) 双重抑制剂,作用于 AurA (IC50: 6.9 nM) 和 PKCα (IC50: 16.9 nM)。Aurora A/PKC-IN-1 对乳腺癌细胞表现出抗增殖和抗转移作用。
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。
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].
T71112 SAR156497

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expressi...
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.
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。
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-1aurora 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。
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。
T6936 PF-03814735

FAK; VEGFR; FLT; Trk receptor; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
PF-03814735 是一种新型、有效和可逆的极光激酶 A 和 B 抑制剂,IC50值分别为0.8和5 nM。
T79913 GRK2 Inhibitor 2

GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂,对GRK2有显著的抑制活性(IC50: 19 nM),同样对Aurora-A也表现出抑制作用(IC50: 137 nM)。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外,GRK2 Inhibitor 2适用于充血性心力衰竭(HF)的相关研究。
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...
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 Cdk1Aurora 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。

化合物

Aurora inhibitor 1
Cat.No: T10412
Synonym:
Target: Aurora Kinase
Aurora B inhibitor 1
Cat.No: T12010
Synonym:
Target: Aurora Kinase
Aurora A inhibitor 1
Cat.No: T63436
Synonym:
Target:
Chiauranib
Cat.No: T35570
Synonym: CS2164,西奥罗尼
Target: c-Fms, VEGFR, FLT, PDGFR, c-Kit, Aurora Kinase
CCT129202
Cat.No: T6435
Synonym: 2-[4-[6-氯-2-(4-二甲基氨基苯基)-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]-N-(噻唑-2-基)乙酰胺
Target: Aurora Kinase
PF 477736
Cat.No: T6028
Synonym: PF 00477736,PF-477736,PF-736,PF-00477736,PF477736
Target: c-Fms, VEGFR, FGFR, FLT, c-RET, Chk, CDK, Src, Aurora Kinase
Ilorasertib hydrochloride
Cat.No: T11638
Synonym: ABT-348 hydrochloride
Target: Aurora Kinase
Aurora kinase inhibitor-3
Cat.No: T5524
Synonym: Aurora Kinase Inhibitor III
Target: Aurora Kinase
Ilorasertib
Cat.No: TQ0059
Synonym: ABT-348
Target: VEGFR, FLT, c-RET, PDGFR, Aurora Kinase
AMG 900
Cat.No: T6380
Synonym: AMG900,AMG-900,莪术醇.姜黄醇
Target: p38 MAPK, Tyrosine Kinases, Aurora Kinase
AT9283
Cat.No: T3068
Synonym: J-504568
Target: Apoptosis, FLT, JAK, Bcr-Abl, Aurora Kinase, Autophagy
GSK-1070916
Cat.No: T6129
Synonym: GSK-1070916A,GSK1070916
Target: Apoptosis, Tie-2, FLT, AMPK, Aurora Kinase
CYC-116
Cat.No: T6458
Synonym: 噻氯匹定
Target: VEGFR, FLT, CDK, S6 Kinase, Aurora Kinase
TAK-285
Cat.No: T6039
Synonym: TAK285,TAK 285
Target: EGFR, MEK, HER, Aurora Kinase
AKI603
Cat.No: T64338
Synonym: AKI 603,AKI-603
Target: Aurora Kinase
XMD-12
Cat.No: T71169
Synonym:
Target:
Aurora A/PKC-IN-1
Cat.No: T62945
Synonym:
Target:
Aurora/LIM kinase-IN-1
Cat.No: T60783
Synonym:
Target:
GSK2646264
Cat.No: T61527
Synonym:
Target:
SAR156497
Cat.No: T71112
Synonym:
Target:
NVP-TAC544
Cat.No: T68740
Synonym:
Target:
Aurora Kinases-IN-4
Cat.No: T78753
Synonym:
Target: Aurora Kinase
CD532 hydrochloride
Cat.No: T36932
Synonym:
Target:
Aurora kinase-IN-1
Cat.No: T72522
Synonym:
Target:
Aurora A inhibitor 3
Cat.No: T82931
Synonym:
Target: Aurora Kinase
PF-03814735
Cat.No: T6936
Synonym:
Target: FAK, VEGFR, FLT, Trk receptor, Aurora Kinase
GRK2 Inhibitor 2
Cat.No: T79913
Synonym:
Target:
AZD 1152 (hydrochloride)
Cat.No: T36199
Synonym:
Target:
JH295 hydrate
Cat.No: T61061
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2718 Palmatine chloride

Others; Indoleamine 2,3-Dioxygenase (IDO); Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic; Metabolism; Others
Palmatine chloride 是口服具有活力的不可逆 IDO-1抑制剂。它能够减轻结肠损伤,预防肠道菌群失调和调节色氨酸分解代谢,并改善 DSS 诱发的结肠炎。
T5S0802 Palmatine

巴马汀,Berbericinine,Burasaine

Indoleamine 2,3-Dioxygenase (IDO); AChR; AChE; Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic; Metabolism; Neuroscience
Palmatine (Burasaine) 是口服具有活力的、不可逆IDO-1抑制剂。它可以减轻结肠损伤,预防肠道菌群失调和调节色氨酸分解代谢,从而改善DSS (Dextran Sulphate Sodium Salt) 诱发的结肠炎。它有用于结肠炎的研究潜力。

天然产物

Palmatine chloride
Cat.No: T2718
Synonym:
Target: Others, Indoleamine 2,3-Dioxygenase (IDO), Aurora Kinase
Palmatine
Cat.No: T5S0802
Synonym: 巴马汀,Berbericinine,Burasaine
Target: Indoleamine 2,3-Dioxygenase (IDO), AChR, AChE, Aurora Kinase
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