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36

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22661	CHM-1	Apoptosis; Others; Microtubule Associated	Apoptosis; Cytoskeletal Signaling; Others
	CHM-1 是细胞凋亡的诱导剂，通过激活 Cdc2 激酶活性在人肝细胞癌中显示出有效的抗肿瘤能力。 CHM-1 在体外和体内抑制微管蛋白聚合。
T21588	Olomoucine	ERK; CDK	Cell Cycle/Checkpoint; MAPK
	Olomoucine 是 Cdk2/cyclin A、Cdc2/CyclinB、CDK2/CyclinE、CDK5/p35 和 ERK1/p44 MAP 激酶的 ATP 竞争性抑制剂，IC50 分别为 7、7、7、3 和 25 µM。 Olomoucine 调节细胞周期并表现出抗黑色素肿瘤活性。
T2028	NG 52 NG52,NG-52,Compound 52	CDK	Cell Cycle/Checkpoint
	NG 52 (NG-52) 是可逆和 ATP 相容性且具有口服活性的Cdc28p 和Pho85p 激酶抑制剂，IC50分别为 7 μM 和 2 μM。它还抑制磷酸甘油酸激酶 1 的活性，IC50值为 2.5 μM。
T7167	Purvalanol B NG 95,(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇	CDK; Parasite	Cell Cycle/Checkpoint; Microbiology/Virology
	Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。
T10723	CDC25B-IN-1 ethyl 3-[(3-methoxynaphthalen-1-yl)amino]benzoate	Phosphatase	Metabolism
	CDC25B-IN-1 是 CDC25B 的抑制剂，Ki 为 8.5 μM。 CDC25B-IN-1 通过抑制细胞增殖和集落形成来增加 G2/M 期。
T9156	CDC25B-IN-2	Phosphatase; mTOR	Metabolism; PI3K/Akt/mTOR signaling
	BIA 是一种 cdc25B 抑制剂。
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。
T82762	Cdc25A (80-93) (human)
	Cdc25A (80-93) (human)为调控细胞周期蛋白D1及G1/S转换中相关蛋白表达，进而控制细胞增殖与肿瘤发生的多肽。该化合物在癌症研究中具应用价值。
T2670	ML167 NCGC00188654,CID44968231	DYRK; CDK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	ML167 (CID44968231) 是一种高选择性的 Cdc2 样激酶 4 抑制剂，IC50为 136 nM。
T1901	(E/Z)-TG003 TG003	BCL; CDK	Apoptosis; Cell Cycle/Checkpoint
	(E/Z)-TG003 是一种有效的 ATP 竞争性 Cdc2 样激酶 (Clk) 抑制剂，抑制 Clk1 和 Clk4 的 IC50值分别为 20 和 15 nM。它是 (Z)-TG003 和 (E)-TG003的消旋体。
T2059	Purvalanol A NG-60	Apoptosis; CDK; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint
	Purvalanol A (NG-60) 是一种CDK 抑制剂，对 cdc2-cyclin B、cdc2-cyclin B、cdk2-cyclin E、cdk4-cyclin D1 和 cdk5-p35 的IC50值分别为 4、70、35、850 和 75 nM。
T3074	CHIR 98024 CHIR98014	GSK-3; S6 Kinase	MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	CHIR 98024是一种有效的 GSK-3α/β 抑制剂，在无细胞试验中 IC50 为 0.65 nM/0.58 nM，能够区分 GSK-3 与其接近的同源物 Cdc2 和 ERK2。
T2095	Seliciclib Roscovitine,R-roscovitine,CYC202	CDK	Cell Cycle/Checkpoint
	Seliciclib (Roscovitine) 是 Cdk2/cyclin E 的有效抑制剂，IC50为0.1 µM。它还抑制 Cdk7/cyclin H、Cdk5/p35 和 Cdc2/cyclin B，IC50为 0.49、0.16和0.65 µM。
T15438	GSK3186899 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide,DDD-853651	Parasite	Microbiology/Virology
	GSK3186899 是 Cdc2 相关激酶 12 的抑制剂，对 L. donovani 的 EC50 为 1.4 μM。
T6350	CHIR-124 CHIR124,CHIR 124	Apoptosis; GSK-3; FLT; Chk; PDGFR; Src	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	CHIR-124 是一种选择性 Chk1抑制剂，IC50值为 0.3 nM，可有效抑制 PDGFR 和 FLT3，IC50值分别为 6.6 nM 和 5.8 nM。
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。
T2310L	CHIR-99021 HCl CT99021 HCl,Laduviglusib HCl	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂，IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性，对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外，CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外，它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外，拉杜维格西单盐酸盐诱导自噬[1][2][3]。
T2608	CHIR-98014 CHIR 98014,CT98014,CHIR98014	FGFR; GSK-3; Src; S6 Kinase	Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	CHIR-98014 (CT98014) 是有效的，细胞通透的GSK-3抑制剂，可抑制 GSK-3α (IC50:0.65 nM) 和 GSK-3β (IC50:0.58 nM) 的活性，对 cdc2 和 erk2 的作用较弱。
T10836	CLK1-IN-1	CDK	Cell Cycle/Checkpoint
	CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).
T15657	KH-CB19	Others	Others
	KH-CB19 is an effective and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).
T24402	Leucettine L41 LeucettineL41,Leucettine-L41
	Leucettine L41 is an effective dual cdc2-like kinase and DYRKs inhibitor.
T16848	SB-218078	Chk; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling
	SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).
T22657	Laduviglusib trihydrochloride CT99021 trihydrochloride,CHIR 99021 trihydrochloride,CHIR 99021 trihydrochloride (252917-06-9 free base)	GSK-3; Wnt/beta-catenin	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells
	Laduviglusib trihydrochloride (CT99021 trihydrochloride) 是一种选择性糖原合成酶激酶 3 (GSK-3) 抑制剂，对 GSK-3α 和 GSK-3β 的 IC50 分别为 10 nM 和 6.7 nM。 Laduviglusib trihydrochloride 抑制人 GSK-3β，Ki 为 9.8 nM。 Laduviglusib trihydrochloride 是 Wnt/β-catenin 信号通路的激活剂。 Laduviglusib trihydrochloride 诱导自噬。
T68453	HY-52
	HY-52 is a selective inhibitor of CDC2 kinase.
T62049	CTX-712
	CTX-712 是有效的cdc2 样激酶 (CLK) 抑制剂。CTX-712 可以抑制癌症存活和癌细胞生长。
T70527	DAT-230
	DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated ...
T69091	CBP501
	CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.
T69316	DA 3003-2 NSC663285
	DA 3003-2为一种高效的选择性Cdc25抑制剂，展示了抗增殖活性，能诱导细胞周期在G2/M期停滞，并提高P-tyr15Cdc2表达量，显示出对前列腺癌研究的应用潜力。
T60737	LG308
	LG308 是一种新型合成化合物，具有抗微管活性。LG308 诱导细胞凋亡和细胞死亡，并且显著抑制肿瘤生长，具有前列腺癌的研究潜力。LG308 诱导有丝分裂阻滞并显着抑制 G2/M 的进程，这与细胞周期蛋白 B1 和有丝分裂标志物 MPM-2 的上调以及 cdc2 的去磷酸化有关。
T28092	MPT0B206
	MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2.
T21950	K 00546
	K00546 是一种有效的细胞周期蛋白依赖性激酶CDK1和CDK2抑制剂，对CDK1/cyclin B 和CDK2/cyclin A 的IC50分别为 0.6 nM 和 0.5 nM。K00546 也是一种有效的 CDC2 样激酶 1 (CLK1) 和CLK3抑制剂，IC50分别为 8.9 nM 和 29.2 nM。
T71217	MPT0B214
	MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of th...
TP2192	Cdk2/Cyclin Inhibitory Peptide I	Others	Others
	Cyclin-dependent kinase 2 also known as cell division protein kinase 2. The protein encoded by this gene is a member of the cyclin-dependent kinase family of Ser/Thr protein kinases. This protein kinase is highly similar to the gene products of S. cerevis
T69200	CGP74514A
	CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and...
T62484	Aurora Kinases-IN-2
	Aurora Kinases-IN-2 (compound 12Aj) 是一种 Aurora 激酶的有效抑制剂 (Aurora kinases)，能够作用于 Aurora A (IC50: 90 nM) 和 Aurora B (IC50: 152 nM)。Aurora Kinases-IN-2 能够调节细胞周期蛋白 B1 和 cdc2 ，将细胞周期阻滞在 G2/M 期。Aurora Kinases-IN-2 能够用于研究癌症。
T36689	KuWal151
	Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

化合物

Cat.No: T22661

Target: Apoptosis, Others, Microtubule Associated

Cat.No: T21588

Target: ERK, CDK

Cat.No: T2028

Synonym: NG52,NG-52,Compound 52

Target: CDK

Cat.No: T7167

Synonym: NG 95,(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇

Target: CDK, Parasite

Cat.No: T10723

Synonym: ethyl 3-[(3-methoxynaphthalen-1-yl)amino]benzoate

Target: Phosphatase

Cat.No: T9156

Target: Phosphatase, mTOR

P34cdc2 Kinase Fragment

Cat.No: T76458

Cdc25A (80-93) (human)

Cat.No: T82762

Cat.No: T2670

Synonym: NCGC00188654,CID44968231

Target: DYRK, CDK

Cat.No: T1901

Synonym: TG003

Target: BCL, CDK

Cat.No: T2059

Synonym: NG-60

Target: Apoptosis, CDK, Autophagy

Cat.No: T3074

Synonym: CHIR98014

Target: GSK-3, S6 Kinase

Cat.No: T2095

Synonym: Roscovitine,R-roscovitine,CYC202

Target: CDK

Cat.No: T15438

Synonym: 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide,DDD-853651

Target: Parasite

Cat.No: T6350

Synonym: CHIR124,CHIR 124

Target: Apoptosis, GSK-3, FLT, Chk, PDGFR, Src

Cat.No: T9864

Synonym: WEE1-IN-5

Target: Wee1

Cat.No: T2310L

Synonym: CT99021 HCl,Laduviglusib HCl

Target: GSK-3

Cat.No: T2608

Synonym: CHIR 98014,CT98014,CHIR98014

Target: FGFR, GSK-3, Src, S6 Kinase

Cat.No: T10836

Target: CDK

Cat.No: T15657

Target: Others

Cat.No: T24402

Synonym: LeucettineL41,Leucettine-L41

Cat.No: T16848

Target: Chk, PKC

Laduviglusib trihydrochloride

Cat.No: T22657

Synonym: CT99021 trihydrochloride,CHIR 99021 trihydrochloride,CHIR 99021 trihydrochloride (252917-06-9 free base)

Target: GSK-3, Wnt/beta-catenin

Cat.No: T68453

Cat.No: T62049

Cat.No: T70527

Cat.No: T69091

Cat.No: T69316

Synonym: NSC663285

Cat.No: T60737

Cat.No: T28092

Cat.No: T21950

Cat.No: T71217

Cdk2/Cyclin Inhibitory Peptide I

Cat.No: TP2192

Target: Others

Cat.No: T69200

Aurora Kinases-IN-2

Cat.No: T62484

Cat.No: T36689

Cat. No.	Product Name	Target	Signaling Pathways
T25192	Butyrolactone I Olomoucin,丁酸内酯I	CDK	Cell Cycle/Checkpoint
	Butyrolactone I (Olomoucin) 是 CDK 和 cdc2 激酶家族的 ATP 竞争性抑制剂。 Butyrolactone I 在非小细胞肺、小细胞肺和前列腺癌细胞系中显示出抗肿瘤作用。
T5S1467	Cucurbitacin E	CDK; Autophagy	Autophagy; Cell Cycle/Checkpoint
	Cucurbitacin E 是从黄瓜的攀缘茎中分离得到的一种天然产物。它显着抑制细胞周期蛋白B1/CDC2复合物的活性，具有预防神经变性，具有强效的抗增殖、抗肿瘤、抗炎和镇痛作用行动。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。
TN5639	Rocaglaol Ferrugin,Aglaiastatin A
	Rocaglaol is a potent anticancer drug that induces apoptosis of LNCaP cells through the mitochondrial pathway and its G2/M-phase cell cycle arrest is associated with the down-regulation of Cdc25C and the dephosphorylation of Cdc2. Rocaglaol can reduce tis

天然产物

Butyrolactone I

Cat.No: T25192

Synonym: Olomoucin,丁酸内酯I

Target: CDK

Cat.No: T5S1467

Target: CDK, Autophagy

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

Cat.No: TN5639

Synonym: Ferrugin,Aglaiastatin A

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