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37

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2134	c-JUN peptide
	Peptide comprising residues 33 - 57 of the JNK binding (δ) domain of human c-Jun. Disrupts JNK/c-Jun interaction leading to inhibition of serum-induced c-Jun phosphorylation, up-regulation of p21cip/waf and modulation of inflammatory gene expression. Spec
T33467	MOMIPP	PI3K	PI3K/Akt/mTOR signaling
	MOMIPP 是一种 PIKfyve 抑制剂，是一种巨胞饮作用的诱导剂，可穿过血脑屏障 (BBB)。
T12189	NBDHEX	Apoptosis; Glutathione Peroxidase; Autophagy	Apoptosis; Autophagy; Metabolism
	NBDHEX 是一种谷胱甘肽 S-转移酶 P1-1 抑制剂，也是晚期自噬抑制剂。它诱导肿瘤细胞凋亡，通过抑制 GST 的催化活性，避免抑制剂被特异性泵从细胞中排出，以及破坏 GSTP1-1和关键信号传导因子之间的相互作用，从而起到抗癌的作用。
T9688	CC-90001	JNK	MAPK
	CC-90001 是口服有效的 c-Jun N 末端激酶选择性抑制剂。在基于细胞的模型中，CC-90001显示出对JNK1的选择性是JNK2的 12.9 倍。CC-90001在特发性肺纤维化方面有研究价值。
T9052	XL092 CL-092,JUN04542	VEGFR; c-Met/HGFR; TAM Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	XL092 (JUN04542) 是一种ATP 竞争性的、口服有效的多受体酪氨酸激酶 (RTKs) 抑制剂，在细胞分析中的MET (IC50:15 nM)、VEGFR2 (IC50:1.6 nM)、AXL (IC50:3.4 nM) 和 MER (IC50:7.2 nM)。它具有抗肿瘤作用，具有用于研究激酶依赖性疾病的潜力。
T5097	Ezatiostat TER199(free base),TLK199	Apoptosis; Glutathione Peroxidase; GST	Apoptosis; Metabolism; oxidation-reduction
	Ezatiostat (TER199(free base)) 是一种谷胱甘肽的三肽类似物，也是一种选择性的口服活性的谷胱甘肽 S-转移酶 P1-1 (GSTP1) 抑制剂。它通过抑制GSTP1导致 JNK 激活，刺激淋巴细胞生成和骨髓祖细胞增殖，可研究骨髓增生异常综合症。
T9010	IMM-H007	Others; AMPK	Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling
	IMM-H007 是一种新型降脂剂，可增加 abca1 蛋白的表达。
T22776	Ezatiostat hydrochloride TLK199 HCl,Ezatiostat盐酸盐,TER199	Glutathione Peroxidase	Metabolism
	Ezatiostat hydrochloride (TLK199 HCl) 是一种新型谷胱甘肽类似物，可刺激淋巴细胞生成和骨髓祖细胞增殖，可用于治疗血细胞减少症和研究骨髓增生异常综合症。它也是口服活性的选择性谷胱甘肽 S-转移酶 P1-1 抑制剂，通过抑制 GSTP1导致 JNK 激活。
T2343	AS601245	JNK	MAPK
	AS601245 是 c-Jun NH2-末端激酶 (JNK) 的抑制剂，具有神经保护特性。
T5416	T-5224	MMP	Proteases/Proteasome
	T-5224 是选择性的转录因子c-Fos/activator protein (AP)-1抑制剂，具有抗炎作用，能够特异性抑制 c-Fos/c-Jun 的 DNA 结合活性，但对其他转录因子的结合活性无影响。它抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。
T7677	JNK Inhibitor VIII TCS JNK 6o	JNK	MAPK
	JNK Inhibitor VIII (TCS JNK 6o) 是一种 c-Jun N-末端激酶(JNK-1, -2, -3)抑制剂，对 JNK-1、JNK-2 的IC50值分别是 45 nM 和 160 nM，对JNK-1、JNK-2、JNK-3 的Ki 分别为 2 nM、4 nM、52 nM。
T3598	JNK-IN-7 JNK inhibitor	JNK	MAPK
	JNK-IN-7 (JNK inhibitor) 是 JNK 抑制剂，抑制 JNK1、JNK2和 JNK3，IC50分别为 1.5、2 和 0.7 nM。
T5833	CC-401 Hydrochloride CC401 HCl	JNK	MAPK
	CC-401 Hydrochloride (CC401 HCl) 是 JNK 抑制剂(Ki= 25~50 nM)。
T68060	Elgodipine
	Elgodipine 显著降低了运动诱导的心绞痛系统的发生率和严重程度，能够通过独立于转录因子c-fos 和c-jun 表达的机制抑制血管平滑肌增殖。 Elgodipine 诱导的抑制是电压依赖性的。Elgodipine 是治疗心绞痛的潜在化合物。
T16436	PBOX 6 PBOX-6	Apoptosis	Apoptosis
	PBOX 6 是一种 pyrrolo-1,5-benzoxazepine (PBOX) 化合物，具有抗癌抗肿瘤活性，可在体外抑制乳腺癌细胞的生长，在白血病细胞中通过 c-Jun NH2 末端激酶依赖性磷酸化、 Bcl-2 和 Bcl-XL 的失活发生选择性诱导细胞凋亡。
TP1897L1	JIP-1 (153-163) acetate(438567-88-5 free base)	JNK	MAPK
	JIP-1 (153-163) acetate(438567-88-5 free base) 是c-Jun N-末端激酶 (JNK) 的肽抑制剂，基于 JNK-interacting protein-1 (JIP-1) 的残基 153-163。以微摩尔范围内的亲和力与 JNK 结合，并抑制 p38 和 ERK。
T73457	DN-1289	DNA Alkylation	DNA Damage/DNA Repair
	DN-1289 是一种可口服可通过血脑屏障且具有选择性高效性的抑制剂，对双亮氨酸拉链激酶 (DLK）的 IC50 值为17 nM，对亮氨酸拉链轴承激酶 (LZK）的 IC50 值为 40 nM。DN-1289 对小鼠模型中视神经挤压 (ONC) 诱导的 p-c-Jun 有显著的抑制作用。
T3627	IQ-1S free acid IQ-1,IQ-1S,IQ-1S (free acid)	NF-κB; JNK	MAPK; NF-κB
	IQ-1S free acid (IQ-1S) 是 NF-κB/激活蛋白1 (AP-1) 抑制剂(IC50:2.3±0.41 μM)。它对 JNK1(Kd:240 nM)、JNK2(Kd:360 nM) 和 JNK3(Kd:100 nM)的都具有高的结合亲和力。
T8505	SC-236 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236	Apoptosis; COX; PPAR	Apoptosis; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience
	SC-236 (Sc 236) 是一种具有口服活性的COX-2特异性抑制剂和PPARγ激动剂。它可通过 c-Jun 氨基端抑制激活蛋白-1活性，在小鼠模型中通过抑制 ERK 的磷酸化发挥抗炎作用。
T24830	SR-4326
	SR-4326 is a c-Jun N-terminal Kinase 3 inhibitor.
T13779	MPT0B392	Others	Others
	MPT0B392 is an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation.
T69527	Erioflorin
	Erioflorin is an ATP-competitive selective c-Jun N-terminal kinase (JNK) inhibitor.
T29590	Acetoxycycloheximide
	Acetoxycycloheximide induces cell surface TNF receptor 1. It also rapidly induces apoptosis mediated by the release of cytochrome c via activation of c-Jun N-terminal kinase.
T81036	TAT-JIP
	TAT-JIP抑制了PHA–PMA诱导的内源性c-jun的磷酸化作用。
T16721	Ralimetinib LY2228820	Others	Others
	Ralimetinib selectively inhibits phosphorylation of MK2 (Thr334) and has no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib is an effective and selective, ATP-competitive inhibitor of p38 MAPK α/β (IC50s: 5.3 and 3.
T11702	J30-8	Others	Others
	J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases. J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivit
TP1897	JIP-1(153-163) JIP-1 (153-163)
	JIP-1(153-163) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1(153-163) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.
T39586	Cantrixil TRX-E-002-1
	Cantrixil (TRX-E-002-1) is a second-generation super-benzopyran (SBP) compound, derived from TRX-E-002. It elicits an increase in phosphorylated c-Jun levels, leading to caspase-mediated apoptosis in ovarian cancer cells. Cantrixil exhibits potent pan anti-cancer activity against various cancer phenotypes.
T36673	CC 401 dihydrochloride
	High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 \|Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J...
T72714	JNK3 inhibitor-3	JNK	MAPK
	JNK3inhibitor-3（compound 15g）是一种选择性的c-Jun N-terminal kinase3（JNK3）抑制剂，具有良好的血脑屏障穿透性和口服生物利用度。其对JNK1、JNK2和JNK3的IC50分别为147.8 nM、44.0 nM和4.1 nM。在小鼠痴呆模型中，JNK3inhibitor-3能显著改善记忆功能，因此有望作为阿尔茨海默病研究的工具化合物。
T79489	JNK-1-IN-2	JNK	MAPK
	JNK-1-IN-2（Compound c6）是一种选择性JNK-1抑制剂，其IC50值为33.5 nM。同时，该化合物对JNK-2和JNK-3也具有抑制作用，其IC50值分别为112.9 nM和33.2 nM。通过抑制c-Jun蛋白的磷酸化，JNK-1-IN-2能够逆转肺部损伤，并且可以被应用于肺纤维化的相关研究。
T35943	15(S)-HpETE
	15(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of 15-lipoxygenase (15-LO) on arachidonic acid. It is either metabolized to 14,15-leukotriene A4 [1] or reduced to 15(S)-HETE by peroxidases.[2] [1] 15(S)-HpETE mediates a number of biological functions including the induction of c-fos and c-jun, and activation of AP-1. [3] 15(S)-HpETE inhibits prostacyclin synthesis in porcine aortic microsomes and bovine endothelial cells, and can cause the suicide inac...
T37969	12(S)-HpETE
	12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LO, resulting in the synthesis of 5(S)-HETE, leukotriene B4 (LTB4), and 5(S),12(S)-DiHETE. Rat lung metabolizes 12(S)-HpETE to 8,11,12- and 10,11,12-trihydroxyeicostrienoic acids. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and e...
T37458	C18 Phytoceramide (t18:0/18:0)
	C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in S. cerevisiae, wheat grains, and the stratum corneum layer of mammalian epidermis. Cer(t18:0/18:0) is composed of a phytosphingosine backbone amine-linked to a C18 fatty acid chain. Cer(t18:0/18:0) has a role in regulation of apoptosis, cell differentiation, proliferation of smooth muscle cells, and inhibition of the mitochondrial respiratory chain. It also inhibits expression of the allergic cytokines IL-4, TN...
T36346	Ac-VEID-AMC (ammonium acetate salt)
	Ac-VEID-AMC is a fluorogenic substrate based on the caspase-6 cleavage site in lamin A at amino acids VEID during apoptosis.1It has also been reported to be cleaved by related proteases, including caspase-8.2Caspase activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. 1.Talanian, R.V., Quinlan, C., Trautz, S., et al.Substrate specificities of caspase family proteasesJ. Biol. Chem.272(15)9...
T38269	Purfalcamine
	Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...

化合物

c-JUN peptide

Cat.No: TP2134

Cat.No: T33467

Target: PI3K

Cat.No: T12189

Target: Apoptosis, Glutathione Peroxidase, Autophagy

Cat.No: T9688

Target: JNK

Cat.No: T9052

Synonym: CL-092,JUN04542

Target: VEGFR, c-Met/HGFR, TAM Receptor

Cat.No: T5097

Synonym: TER199(free base),TLK199

Target: Apoptosis, Glutathione Peroxidase, GST

Cat.No: T9010

Target: Others, AMPK

Ezatiostat hydrochloride

Cat.No: T22776

Synonym: TLK199 HCl,Ezatiostat盐酸盐,TER199

Target: Glutathione Peroxidase

Cat.No: T2343

Target: JNK

Cat.No: T5416

Target: MMP

JNK Inhibitor VIII

Cat.No: T7677

Synonym: TCS JNK 6o

Target: JNK

Cat.No: T3598

Synonym: JNK inhibitor

Target: JNK

CC-401 Hydrochloride

Cat.No: T5833

Synonym: CC401 HCl

Target: JNK

Cat.No: T68060

Cat.No: T16436

Synonym: PBOX-6

Target: Apoptosis

JIP-1 (153-163) acetate(438567-88-5 free base)

Cat.No: TP1897L1

Target: JNK

Cat.No: T73457

Target: DNA Alkylation

IQ-1S free acid

Cat.No: T3627

Synonym: IQ-1,IQ-1S,IQ-1S (free acid)

Target: NF-κB, JNK

Cat.No: T8505

Synonym: 4-(5-(4-氯苯基)-3-(三氟甲基)-1H-,Sc 236

Target: Apoptosis, COX, PPAR

Cat.No: T24830

Cat.No: T13779

Target: Others

Cat.No: T69527

Acetoxycycloheximide

Cat.No: T29590

Cat.No: T81036

Cat.No: T16721

Synonym: LY2228820

Target: Others

Cat.No: T11702

Target: Others

Cat.No: TP1897

Synonym: JIP-1 (153-163)

Cat.No: T39586

Synonym: TRX-E-002-1

CC 401 dihydrochloride

Cat.No: T36673

JNK3 inhibitor-3

Cat.No: T72714

Target: JNK

Cat.No: T79489

Target: JNK

Cat.No: T35943

Cat.No: T37969

C18 Phytoceramide (t18:0/18:0)

Cat.No: T37458

Ac-VEID-AMC (ammonium acetate salt)

Cat.No: T36346

Cat.No: T38269

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat. No.	Product Name	Target	Signaling Pathways
T0518	Methacycline hydrochloride Rondomycin,盐酸甲烯土霉素,盐酸美他环素,Methacycline HCl	ribosome; Antibacterial; Antibiotic	Microbiology/Virology
	Methacycline hydrochloride (Rondomycin) 是四环素抗生素，可抑制细菌蛋白质的合成。它是上皮-间质转化 (EMT) 抑制剂。它在体外可阻断 EMT，体内抑制纤维发生，不会直接影响 TGF-β1 Smad 信号传导。它是抗菌剂，有潜力研究肺纤维化。
T3755	Pinostilbene	Others	Others
	Pinostilbene 是一种 Pterostilbene 的主要代谢物，能够抑制结肠癌细胞。
T3892	Isoacteoside 异麦角甾苷,Isoverbascoside	NF-κB	NF-κB
	Isoacteoside 具有抗炎作用，通过作用于 caspase-1、丝裂原活化蛋白激酶（c-Jun N-末端激酶、p38、细胞外信号调节蛋白激酶）和核因子-kappa B 途径介导。
T3908	10-Gingerol 10-姜酚	Apoptosis	Apoptosis
	10-Gingerol 是一种姜根脂的主要刺激性成分，具有抗炎、抗氧化和抗增殖作用，能够抑制 MDA-MB-231 肿瘤细胞的增殖(IC50:12.1 μM)。
TWS1977	Kamebakaurin 尾叶香茶菜丙素,Kamebakaurine	NF-κB	NF-κB
	Kamebakaurin (Kamebakaurine) 是一种提取自Isodon japonicus 中的天然产物，是一种NF-κB 的抑制剂，能够抑制 p50 的 DNA 结合活性。
T6S1597	Mulberroside A 桑皮苷 A,桑皮苷A	TNF; Tyrosinase; Interleukin	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Mulberroside A 是桑中的一种主要活性成分，可降低TNF-α、IL-1β和IL-6的表达，抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。它抑制蘑菇酪氨酸酶，具有抗炎和抗细胞凋亡作用。
T6S1572	Sauchinone	ERK; p38 MAPK; NF-κB	MAPK; NF-κB
	Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS，TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。

天然产物

Methacycline hydrochloride

Cat.No: T0518

Synonym: Rondomycin,盐酸甲烯土霉素,盐酸美他环素,Methacycline HCl

Target: ribosome, Antibacterial, Antibiotic

Cat.No: T3755

Target: Others

Cat.No: T3892

Synonym: 异麦角甾苷,Isoverbascoside

Target: NF-κB

Cat.No: T3908

Synonym: 10-姜酚

Target: Apoptosis

Cat.No: TWS1977

Synonym: 尾叶香茶菜丙素,Kamebakaurine

Target: NF-κB

Cat.No: T6S1597

Synonym: 桑皮苷 A,桑皮苷A

Target: TNF, Tyrosinase, Interleukin

Cat.No: T6S1572

Target: ERK, p38 MAPK, NF-κB

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