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26

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40577	TAK1-IN-3	MAPK	MAPK
	TAK1-IN-3 是一种新型 ATP 竞争性 TAK1 抑制剂，可用于研究癌症。
T36782	TAK1-IN-2 TAK1-IN-2
	TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.
T67909	TAK1 inhibitor compound 13a	Topoisomerase	DNA Damage/DNA Repair
	TAK1 inhibitor 是一种抑制剂，对MCF-7、A549 、DU-145 、MDA MB-231有抑制作用，IC50分别为 0.021、0.14、0.064 、0.19 。化合物13 具有较好的抑菌活性,麦克风范围为93.7 ~ 46.9μg / mL,麦克风范围为7.8 ~ 5.8μg / mL。
T70741	AZ-TAK1
	AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and...
T10444	TAK1/MAP4K2 inhibitor 1	Others	Others
	TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor of TGFβ-activated kinase 1 (TAK1) and MAP4K2 (IC50s: 41.1 nM and 18.2 nM).
T6150	TAK-715	p38 MAPK; Casein Kinase; JNK	MAPK; Metabolism; Stem Cells
	TAK-715 是一种具有口服活性的p38 MAPK 抑制剂，对 p38α 和 p38β 的IC50分别为 7.1 nM 和200 nM。它抑制酪蛋白激酶 I (CK1δ/ε)，调节 Wnt/β-catenin 信号传导的激活，有抗炎活性。
T70739	KW 4099
	KW 4099 is a thromboxane A2 antagonist.
T4264	Takinib EDHS-206	Apoptosis; MAPK	Apoptosis; MAPK
	Takinib (EDHS-206) 是一种TAK1自磷酸化的抑制剂，也是恶性疟原虫蛋白激酶 9 抑制剂，在 ATP 结合口袋内非竞争性结合。它诱导 TNF-α 刺激的细胞凋亡，可研究类风湿关节炎和转移性乳腺癌。
T62209	HS-276	MAPK	MAPK
	HS-276 是一种高度选择性的、口服具有活力的 TAK1 抑制剂 (Ki: 2.5 nM)。HS-276 能够显著抑制 TAK1 (IC50: 8.25 nM)、CLK2 (IC50: 29 nM)、GCK (IC50: 22 nM)、ULK2 (IC50: 63 nM)、MAP4K5 (IC50: 125 nM)、IRAK1 (IC50: 264 nM)、NUAK (IC50: 270 nM)、CSNK1G2 (IC50: 810 nM)、CAMKKβ-1 (IC50: 1280 nM) 和 MLK1 (IC50: 5585 nM)。HS-276 能够用于研究类风湿关节炎 (RA)。
T5643	NG25	MAPK	MAPK
	NG25 是TAK1(IC50:149 nM)和MAP4K2(IC50:21.7 nM)的双抑制剂。
T60657	(R)-STU104	TNF; MAPK	Apoptosis; MAPK
	(R)-STU104 是一种新型 TAK1-MKK3 蛋白-蛋白相互作用（PPI）抑制剂，抑制 TNF-α，通过与 MKK3 结合并破坏TAK1磷酸化MKK3来抑制TAK1/MKK3/p38/MnK1/MK2/elF4E信号通路。(R)-STU104 是治疗溃疡性结肠炎的候选化合物。
T60011	HS220	MAPK	MAPK
	HS220 是 TAK1 抑制剂，TAK1 在炎症和细胞存活的信号通路中起关键作用。
T5209	INH14	IκB/IKK	NF-κB
	INH14 是 IKKα (IC50:8.97 μM) / IKKβ (IC50:3.59 μM) 的抑制剂。它能够抑制 IKKα/β 依赖性 TLR 炎症反应，抑制 TAK1/TAB1 的下游和 NF-kB 信号通路。它具有抗炎和抗癌作用。
T36680	SM1-71	Serine/threonin kinase; MAPK; LIM Kinase; TGF-beta/Smad; AAK1 (AP2 associated kinase 1)	Cell Cycle/Checkpoint; MAPK; Metabolism; Neuroscience; Stem Cells
	SM1-71 是一种有效的多靶点丙烯酰胺修饰的 TAK1 抑制剂，抑制 MKNK2、MAP2K1/2/3/4/6/7、GAK、AAK1、BMP2K、MAP3K7、MAPKAPK5、GSK3A/B、MAPK1/3、SRC、YES1、FGFR1、ZAK (MLTK)、MAP3K1、LIMK1 和 RSK2。SM1-71 可作为激酶探针，具有抗癌活性，抑制多种癌细胞系的增殖。
T9428	HM43239	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	HM43239 是一种具有口服活性和选择性 FLT3抑制剂，IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其凋亡 (apoptosis)。
T2378	RGB-286638 free base	GSK-3; MEK; JAK; CDK	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	RGB-286638 free base 是一种新型 CDK 抑制剂，抑制cyclin T1-CDK9、cyclin B1-CDK1、cyclin E-CDK2、cyclin D1-CDK4、cyclin E-CDK3和p35-CDK5活性，IC50分别为 1、2、3、4、5 和 5 nM。它也抑制 GSK-3β、TAK1、Jak2 和 MEK1，IC50值分别为 3、5、50和 54 nM。
T36017	PF-05381941
	PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively[1]. PF-05381941 inhibits LPS-stimulated release of TNF-αfrom human peripheralmononuclear (PMN) cells with an IC50 of 8 nM[1]. [1]. Kilty I, et al. TAK1 inhibition in the DFG-out conformation. Chem Biol Drug Des. 2013;82(5):500-505.
T68914	Antibiotic LL Z1640-2
	Antibiotic LL Z1640-2 is an inhibitor against the TAK1 activity.
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.
T63558	IRAK4-IN-21
	IRAK4-IN-21 是选择性的、口服具有活力的、强效的 IRAK4 抑制剂，能够作用于 IRAK4 (IC50: 5 nM) 和 TAK1 (IC50: 56 nM)。IRAK4-IN-21 对 IL-23 的产生表现出有效的抑制作用，其 IC50值为0.17 μM。IRAK4-IN-21 能够用于研究自身免疫性疾病，如斑块状银屑病和银屑病关节炎。
T63559	IRAK4-IN-22
	IRAK4-IN-22 是选择性的、口服具有活力的、强效的 IRAK4 抑制剂，能够作用于 IRAK4 (IC50: 3 nM) 和 TAK1 (IC50: 17 nM)。IRAK4-IN-21 对 IL-23 的产生表现出有效的抑制作用，其 IC50值为0.10 μM。IRAK4-IN-21 能够用于研究自身免疫性疾病，如斑块状银屑病和银屑病关节炎。
T36779	NG 25 (hydrochloride hydrate)
	NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv...
T72658	cRIPGBM chloride
	cRIPGBM chloride是一种口服有效的促凋亡衍生物，针对多形性胶质母细胞瘤(GBM)中的癌症干细胞(CSC)。该化合物通过靶向受体相互作用蛋白激酶2(RIPK2)，诱导caspase 1依赖的细胞凋亡，抑制RIPK2/TAK1的活性，增加RIPK2/caspase 1复合物的形成，表现出强大的体内抗肿瘤效果。
T73196	RGB-286638
	RGB-286638 是一种有效的 CDK 抑制剂，抑制cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3和p35-CDK5活性，IC50分别为 1，2，3，4，5 和 5 nM；同时可抑制GSK-3β，TAK1，Jak2和MEK1，IC50值分别为 3，5，50，和 54 nM。
T69898	NG25 trihydrochloride
	NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration...
T35438	(5E)-7-Oxozeaenol
	(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 \|1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growt...

化合物

Cat.No: T40577

Target: MAPK

Cat.No: T36782

Synonym: TAK1-IN-2

TAK1 inhibitor

Cat.No: T67909

Synonym: compound 13a

Target: Topoisomerase

Cat.No: T70741

TAK1/MAP4K2 inhibitor 1

Cat.No: T10444

Target: Others

Cat.No: T6150

Target: p38 MAPK, Casein Kinase, JNK

Cat.No: T70739

Cat.No: T4264

Synonym: EDHS-206

Target: Apoptosis, MAPK

Cat.No: T62209

Target: MAPK

Cat.No: T5643

Target: MAPK

Cat.No: T60657

Target: TNF, MAPK

Cat.No: T60011

Target: MAPK

Cat.No: T5209

Target: IκB/IKK

Cat.No: T36680

Target: Serine/threonin kinase, MAPK, LIM Kinase, TGF-beta/Smad, AAK1 (AP2 associated kinase 1)

Cat.No: T9428

Target: FLT

RGB-286638 free base

Cat.No: T2378

Target: GSK-3, MEK, JAK, CDK

Cat.No: T36017

Antibiotic LL Z1640-2

Cat.No: T68914

Cat.No: T69091

Cat.No: T63558

Cat.No: T63559

NG 25 (hydrochloride hydrate)

Cat.No: T36779

cRIPGBM chloride

Cat.No: T72658

Cat.No: T73196

NG25 trihydrochloride

Cat.No: T69898

(5E)-7-Oxozeaenol

Cat.No: T35438

Cat. No.	Product Name	Target	Signaling Pathways
TN1134	Euscaphic acid	Apoptosis; LDL; PI3K; DNA/RNA Synthesis; NO Synthase; Prostaglandin Receptor	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; PI3K/Akt/mTOR signaling
	Euscaphic acid 是来源于枣的一种三萜，是DNA 聚合酶抑制剂，可诱导细胞凋亡。它抑制小牛 DNA 聚合酶 α 和大鼠 DNA 聚合酶 β 的IC50值分别为 61 和 108 μM。
T14055	5Z-7-Oxozeaenol FR148083,L783279,LL-Z 1640-2	VEGFR; FLT; MEK; MAPK; PDGFR; Antibiotic; Src	Angiogenesis; MAPK; Microbiology/Virology; Tyrosine Kinase/Adaptors
	5Z-7-Oxozeaenol (FR148083) 是一种天然抗原生动物抑制剂，不可逆的选择性抑制 TAK1和 VEGF-R2，IC50值分别为 8 nM 和 52 nM。
TN2775	2-Methoxystypandrone	MMP; BCL; IκB/IKK; GSK-3; TNF; NOS; NF-κB; Wnt/beta-catenin; COX; JAK; STAT	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-ÎºB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant
T4700	1,3,5-Trihydroxy-4-prenylxanthone
	1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu
TN5153	Torilin	MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
	Torilin 是一种睾酮5α还原酶抑制剂，它（IC50=31.7+/-4.23μM）对5α还原酶的抑制作用强于α-亚麻酸（IC50=160.3+/-24.62μM），但弱于非那雄胺（IC50=0.38+/-0.06μM）。Torilin 具有免疫调节、肝脏保护和抗炎特性，它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症，它可以减轻关节炎的严重程度，改变 dLN 或关节中的白细胞活化，并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成，IC（50）值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性，它可能通过抑制肿瘤侵袭来抑制肿瘤发生，逆转癌细胞的多药耐药性，它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

Cat.No: TN1134

Target: Apoptosis, LDL, PI3K, DNA/RNA Synthesis, NO Synthase, Prostaglandin Receptor

5Z-7-Oxozeaenol

Cat.No: T14055

Synonym: FR148083,L783279,LL-Z 1640-2

Target: VEGFR, FLT, MEK, MAPK, PDGFR, Antibiotic, Src

2-Methoxystypandrone

Cat.No: TN2775

Target: MMP, BCL, IκB/IKK, GSK-3, TNF, NOS, NF-κB, Wnt/beta-catenin, COX, JAK, STAT

1,3,5-Trihydroxy-4-prenylxanthone

Cat.No: T4700

Cat.No: TN5153

Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK

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