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21

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9151 Teplinovivint

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
Teplinovivint 是 wnt/β-catenin 信号通路抑制剂。它具有抗炎作用,对用于肌腱病具有潜在的研究价值。
T13224 Tubulin inhibitor 6

iHAP1

Microtubule Associated Cytoskeletal Signaling
Tubulin inhibitor 6 (iHAP1) 是一种微管蛋白抑制剂,抑制微管蛋白聚合,IC50为 0.87 μM。它抑制多种癌细胞系,抑制 K562 细胞生长,IC50为 840 nM。
T19147 5-ALA benzyl ester hydrochloride

Benzyl-ALA hydrochloride

Others; Endogenous Metabolite Metabolism; Others
5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) 是一种原卟啉前体,可用作光检测器。5-ALA benzyl ester hydrochloride 在结肠癌细胞系中可以诱导原卟啉 IX (PPIX) 的积聚。
T4459 PK11000

DNA Alkylator/Crosslinker DNA Damage/DNA Repair
PK11000 是一种烷化剂,可通过共价半胱氨酸修饰来稳定野生型和突变型p53的 DNA 结合结构域。
T6583 MG-101

ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I

Cysteine Protease; Proteasome Proteases/Proteasome; Ubiquitination
MG-101 (Calpain inhibitor I) 是一种有效的半胱氨酸蛋白酶抑制剂,能够抑制钙蛋白酶I (Ki:190 pM),钙蛋白酶II (Ki:220 pM),组织蛋白酶B (Ki:150 pM)和组织蛋白酶L (Ki:500 pM)。
T5858 Sertindole

Lu 23-174,舍吲哚

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy Autophagy; GPCR/G Protein; Neuroscience
Sertindole (Lu 23-174) 是一种非典型抗精神病药,可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合,Kd 值分别为 2.7、20、0.14 和 6 nM。
T5636 Adavivint

Adavivint (SM04690)

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
Adavivint (Adavivint (SM04690)) (SM04690) 是选择性的典型的Wnt 信号通路抑制剂,在 SW480 细胞中,用高通量 TCF/LEF 报告基因实验,测得EC50=19.5 nM。
T69625 Benitrobenrazide

Hexokinase 2 inhibitor 1

Hexokinase Metabolism
Benitrobenrazide (Hexokinase 2 inhibitor 1) 是一种新型可口服的己糖激酶 2 (HK2) 抑制剂,具有抗癌抗肿瘤活性,通过靶向糖酵解来阻断癌细胞生长。Benitrobenrazide 抑制 SW1990 和 SW480 异种移植模型中的肿瘤生长,可用于研究癌症。
T13807 OSIP-486823

CP248

Microtubule Associated; PKA Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
OSIP-486823(CP248) 是一种新型有效的微管干扰剂,对蛋白激酶 G (PKG) 和微管均具有亲和力。
T73832 Tubulin inhibitor 21

Tubulin inhibitor 21 (compound 6f) 为基于查尔酮与褪黑激素混合的有效tubulin抑制剂。该化合物对SW480细胞展现显著的细胞毒性活性(IC50=0.26 μM),对非恶性细胞的毒性较低。
T71862 GPR120-IN-1

GPR120-IN-1 is a novel GPR120 inhibitor, showing ~90% inhibitory effects on cell growth with micromolar affinities against SW480.
T61946 IMP2-IN-1

IMP2-IN-1 (compound 4) 是有效的IMP2抑制剂,对 IMP2 RNA 的IC50为 81.3-127.5 μM。IMP2-IN-1 降低 SW480 细胞中 IMP2 水平。IMP2-IN-1 显著抑制分化和未分化 Huh7 细胞的活力。
T36684 Ipivivint

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ip...
T39200 β-catenin-IN-37

β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively.
T34120 PQ1

PQ-1,PQ 1

PQ1, as an enhancer of gap junction in SW480 human colorectal cancer cells can act by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.
T78701 Tubulin inhibitor 32

Apoptosis Apoptosis
Tubulin inhibitor 32是一种口服活性的新型微管抑制剂,具有抗增殖和抗肿瘤活性,可抑制微管聚合,可诱导细胞凋亡及在G2/M期引起细胞周期停滞。
T61823 Anticancer agent 63

Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC 50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. In particular, Anticancer agent 63 induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression. Additionally, Anticancer agent 63 demonstrates antioxidative properties [1].
T72548 IGUANA-1 free base

STL5-T-0057

IGUANA-1 free base (STL5-T-0057) 作为ALDH1B1的选择性抑制剂,IC50值达30 nM。在不同条件下,对SW480细胞的生长抑制显示出显著效果,附着状态下IC50值为2.46 μM,而在球形状态下为0.39 μM。因此,IGUANA-1 free base适用于癌症相关研究。
T65994 (6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation...
T78157 PARP-1-IN-3

Apoptosis; PARP Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
PARP-1-IN-3 是一种高效的 PARP-1 抑制剂,对 PARP-1 和 PARP-2 具有抑制作用, IC50 值分别为 0.25 nM 和 2.34 nM。PARP-1-IN-3 具有潜在的抗炎活性,促使细胞凋亡并使细胞周期停滞在 G2/M 期。PARP-1-IN-3 可用于研究与癌症相关的疾病。
T69618 XR3054

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kina...

化合物

Teplinovivint
Cat.No: T9151
Synonym:
Target: Wnt/beta-catenin
Tubulin inhibitor 6
Cat.No: T13224
Synonym: iHAP1
Target: Microtubule Associated
5-ALA benzyl ester hydrochloride
Cat.No: T19147
Synonym: Benzyl-ALA hydrochloride
Target: Others, Endogenous Metabolite
PK11000
Cat.No: T4459
Synonym:
Target: DNA Alkylator/Crosslinker
MG-101
Cat.No: T6583
Synonym: ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I
Target: Cysteine Protease, Proteasome
Sertindole
Cat.No: T5858
Synonym: Lu 23-174,舍吲哚
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy
Adavivint
Cat.No: T5636
Synonym: Adavivint (SM04690)
Target: Wnt/beta-catenin
Benitrobenrazide
Cat.No: T69625
Synonym: Hexokinase 2 inhibitor 1
Target: Hexokinase
OSIP-486823
Cat.No: T13807
Synonym: CP248
Target: Microtubule Associated, PKA
Tubulin inhibitor 21
Cat.No: T73832
Synonym:
Target:
GPR120-IN-1
Cat.No: T71862
Synonym:
Target:
IMP2-IN-1
Cat.No: T61946
Synonym:
Target:
Ipivivint
Cat.No: T36684
Synonym:
Target:
β-catenin-IN-37
Cat.No: T39200
Synonym:
Target:
PQ1
Cat.No: T34120
Synonym: PQ-1,PQ 1
Target:
Tubulin inhibitor 32
Cat.No: T78701
Synonym:
Target: Apoptosis
Anticancer agent 63
Cat.No: T61823
Synonym:
Target:
IGUANA-1 free base
Cat.No: T72548
Synonym: STL5-T-0057
Target:
(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
Cat.No: T65994
Synonym:
Target:
PARP-1-IN-3
Cat.No: T78157
Synonym:
Target: Apoptosis, PARP
XR3054
Cat.No: T69618
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5750 Oxyberberine

氧化小檗碱,Ketoberberine,Berlambine,8-Oxoberberine

Others Others
Oxyberberine (8-Oxoberberine) 是天然的生物碱类物质。
TN5422 Ciwujiatone

Ciwujiatone exhibits significant activities against colon cancer cell lines SW480 and SW620.
TN3925 Eichlerianic acid

HSV Microbiology/Virology
Eichlerianic acid is a trypanocidal compound with an IC50 value of 10 mg/mL. Eichlerianic acid may have antiviral activity against Herpes simplex virus types I and II in vitro. Eichlerianic acid shows weak cytotoxicity (IC50 6.87 to >40 μM) against human cancer cell (HL-60, SMMC-7721, A-549, MCF-7 and SW480).
TN5676 Musellarin B

Musellarin B is cytotoxic toward several of the human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480).
TN2685 2,3,24-Trihydroxy-12-ursen-28-oic acid

Antifection Microbiology/Virology
2α,3α,24-Trihydroxyurs-12-en-28-oic acid, a triterpenoid phytoalexin, shows antifungal activity against the fungus mentioned. It also shows in vitro cytotoxic activity against tumor cell lines including PLC,Hep3B,HepG2,HeLa,SW480,MCF-7 and Bel7402.
TN3250 7-Prenyljacareubin

Others Others
7-Prenyljacareubin shows moderate cytotoxic activity against HL-60, SMMC-7721, A549, MCF-7, and SW480 cell lines.
TN3616 Cedrelone

Apoptosis; MMP; Antifection Apoptosis; Microbiology/Virology; Proteases/Proteasome
Cedrelone 是一种柠檬苦素类化合物,是一种吩嗪生物合成样结构域蛋白 (PBLD) 激活剂。Cedrelone 可诱导癌细胞凋亡 (apoptosis)。Cedrelone 是一种非常有效的细胞凋亡诱导剂,它能导致细胞周期停止。Cedrelone 具有杀虫活性,可抑制 P. saucia 的箭毒生长,并可抑制乳草蝽(Oncopeltus fasciatus)的蜕皮。Cedrelone具有抗肿瘤作用,对SMMC-7721、A-549、MCF-7 和 SW480 等癌细胞株具有显著的细胞毒性。

天然产物

Oxyberberine
Cat.No: T5750
Synonym: 氧化小檗碱,Ketoberberine,Berlambine,8-Oxoberberine
Target: Others
Ciwujiatone
Cat.No: TN5422
Synonym:
Target:
Eichlerianic acid
Cat.No: TN3925
Synonym:
Target: HSV
Musellarin B
Cat.No: TN5676
Synonym:
Target:
2,3,24-Trihydroxy-12-ursen-28-oic acid
Cat.No: TN2685
Synonym:
Target: Antifection
7-Prenyljacareubin
Cat.No: TN3250
Synonym:
Target: Others
Cedrelone
Cat.No: TN3616
Synonym:
Target: Apoptosis, MMP, Antifection
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