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103

抑制剂 & 化合物

18

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Cat. No. Product Name Target Signaling Pathways
T2051 SKLB4771

FLT3-​IN-​1,FLT3-IN-1

FLT Angiogenesis; Tyrosine Kinase/Adaptors
SKLB4771 (FLT3-IN-1) 是一种新型的、高效的 Flt3 抑制剂 (IC50:10nM)。
T4235 Roblitinib

FGF-401

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
Roblitinib (FGF-401) 是一种口服有效的,高选择性的FGFR4抑制剂(IC50:1.9 nM),具有抗癌作用。
T6831 Etretinate

Retinoid,Tegison,Etretinato,Ethyl etrinoate,Ro 10-9359,依曲替酯

Apoptosis; Others Apoptosis; Others
Etretinate (Ro 10-9359) 是一种口服芳香族维甲酸,对牛皮癣和其他皮肤病综合征有效。 它激活类视黄醇受体,引起细胞分化的诱导、细胞增殖的抑制和炎症细胞对组织浸润的抑制。
T3352 XL413

cholecystokinin; Casein Kinase; Pim; CDK Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; JAK/STAT signaling; Metabolism; Stem Cells
XL413 是一种口服生物可利用的细胞分裂周期 7 同源物 (CDC7) 激酶抑制剂,具有潜在的抗肿瘤活性,IC50值为 3.4 nM。它对 pMCM 的 EC50值为 118 nM,对 CK2 和 PIM1 的 IC50值分别为 215 和 42 nM。
T6017 Linsitinib

OSI-906,林西替尼

IGF-1R Tyrosine Kinase/Adaptors
Linsitinib (OSI-906) 是选择性的、有效的、具有口服活性的IGF-1和胰岛素受体(IR)的双重抑制剂,IC50分别为 35 和 75 nM。
T1849 Momelotinib

CYT11387,CYT387,LM-1149

Apoptosis; JAK; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
Momelotinib (LM-1149) 是一种 ATP 竞争性的 JAK1/JAK2抑制剂,IC50值分别为 11 nM/18 nM。
T3623 Cobimetinib

可美替尼,考比替尼,RG7420,XL518,GDC-0973

Apoptosis; MEK Apoptosis; MAPK
Cobimetinib (GDC-0973) 是一种可口服的 MEK1选择性抑制剂,抑制MEK1的IC50为4.2 nM。
T2307 Icotinib Hydrochloride

埃克替尼盐酸盐,盐酸埃克替尼,BPI-2009H

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Icotinib Hydrochloride (BPI-2009H) 是一种口服的基于喹唑啉的表皮生长因子受体 (EGFR) 抑制剂,IC50值为5 nM,具有潜在的抗肿瘤活性。
T12831L SAR405

PI3K; Autophagy Autophagy; PI3K/Akt/mTOR signaling
SAR-405 是一种选择性 PIK3C3/Vps34 抑制剂,IC50为1.2 nM,Kd 为1.5 nM,可防止自噬并与肿瘤细胞中的 MTOR 抑制协同作用。它抑制饥饿或 mTOR 抑制诱导的自噬,具有抗癌活性。
T1574 Etoricoxib

Arcoxia,MK-663,Tauxib,L-791456,Nucoxia,Desvenlafaxine,依托考昔

COX Immunology/Inflammation; Neuroscience
Etoricoxib (MK-663) 是一种合成的非甾体抗炎药 (NSAID),具有解热、镇痛和潜在的抗肿瘤特性。它是可口服的选择性 COX-2抑制剂,对人全血 COX-2 和 COX-1 的 IC50值分别为 1.1 和 116 μM。
T3211 Midostaurin

米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱

Others; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Others
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。
T6334 Ridaforolimus

AP23573,Deforolimus,MK-8669

mTOR; Autophagy Autophagy; PI3K/Akt/mTOR signaling
Ridaforolimus (AP23573) 是亲脂性大环内酯类抗生素雷帕霉素的小分子非前药类似物,具有潜在的抗肿瘤活性。它是一种有效和选择性的 mTOR 抑制剂,在 HT-1080 细胞中抑制 S6 磷酸化的 IC50值为 0.2 nM。
T11096 DRI-C21045

NF-κB NF-κB
DRI-C21045 是一种有效的 CD40-CD40L 协同刺激蛋白-蛋白质相互作用的选择性抑制剂,IC50 为 0.17 μM。它显示对 CD40L 诱导的 NF-κB 活化和 B 细胞增殖的浓度依赖性抑制,IC50分别为 17.1 μM 和 4.5 μM。
T68405 KW-2450 free base

IGF-1R Tyrosine Kinase/Adaptors
KW-2450 free base 是一种 IGF-1R/IR和酪氨酸激酶多重抑制剂 具有抗肿瘤活性。KW-2450 free base 在小鼠 HT-29/GFP 结肠癌异种移植模型中显示出适度的生长抑制活性并抑制 IGF-1 诱导的信号转导。
T50107 ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate

Others Others
ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate 是一种合成化合物,属于姜黄素家族。它通过抑制NF-κB 信号通路参与免疫反应和炎症的调节,通过激活Nrf2信号通路参与抗氧化反应的调节,通过抑制Akt 信号通路参与细胞存活和增殖的调节。
T1185 Rofecoxib

MK 966,罗非昔布,罗非考昔,MK-0966

COX Immunology/Inflammation; Neuroscience
Rofecoxib (MK 966) 是可口服的 COX-2特异性抑制剂,具有抗炎、解热和镇痛特性以及潜在的抗肿瘤特性。在人骨肉瘤细胞和中国仓鼠卵巢细胞中,对人 COX-2 的 IC50值分别为 26 和 18 nM。
T3626 Acalabrutinib

ACP-196,阿可替尼

BTK Angiogenesis; Tyrosine Kinase/Adaptors
Acalabrutinib (ACP-196) 是一种不可逆的、高效的、具有口服活性、选择性的第二代BTK 抑制剂。它与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。它在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。
T14884 CBR-5884

Others; Dehydrogenase Metabolism; Others
CBR-5884 是一种磷酸甘油酸脱氢酶抑制剂,IC50为 33 μM。 它抑制癌细胞中的丝氨酸合成,选择性地抑制黑素瘤和乳腺癌细胞系的增殖,对具有高丝氨酸生物合成活性的癌细胞系有选择性毒性。
T3630 Relugolix

RVT-601,瑞卢戈利,TAK-385

GNRH Receptor GPCR/G Protein
Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比,它对人和猴子的受体具有高亲和力和强拮抗活性,它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病,如子宫肌瘤、子宫内膜异位症、前列腺癌等。
T12009 Telomerase-IN-1

Telomerase DNA Damage/DNA Repair
Telomease-IN-1是一种端粒酶抑制剂(IC50:0.19μM)。Telomease-IN-1通过ER 过度反应(EOR)的内质网应激(ERS)激活hTERT 的表达,然后诱导ERS,导致细胞凋亡。Telomease-IN-1通过表达下游信号分子包括CHOP(CAAT /增强子结合蛋白同源蛋白))和线粒体凋亡途径,导致细胞增殖受到抑制。Telomease-IN-1对端粒酶具有较高的抑制活性,对SMMC-7721细胞具有较高的抗增殖能力,对人正常肝细胞无明显毒性作用。Telomease-IN-1 在异种移植肿瘤模型表现出抗肿瘤活性。
T35610 2,5-dimethyl Celecoxib

Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T26752 BC12

BC 12,BC-12

BC12 exhibits unusually potent immunomodulatory actions on T lymphocyte function, including inhibition of T cell proliferation and IL-2 cytokine production.
T38720 SR-31747 free base

SR-31747 free base is an immunosuppressive and anti-inflammatory sigma ligand that efficiently inhibits cell proliferation through the inhibition of sterol isomerase activity.
T30508 BMS-243117

UNII-MBE6KWV0QI,CHEMBL67237,MBE6KWV0QI

BMS-243117 is an effective selective LCK inhibitor with good cell activity (IC(50)=1.1 microM) and inhibition of T cell proliferation, which has great potential for therapeutic immunosuppression and the treatment of diseases such as rheumatoid arthritis a
T29176 YKL-04-085

YKL 04085,YKL04-085,YKL 04-085,YKL-04085

YKL-04-085 is a potent inhibitor of viral translation. YKL-04-085 has cellular antiviral activity at 35-fold lower concentrations relative to inhibition of host-cell proliferation. YKL-04-085 demonstrated good inhibition of translation of the DENV2(GVD) r
T21298 SNS-314

SNS-314 free base,SNS314,SNS 314

SNS-314, a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity, selectively binds and inhibits AKs A and B, resulting in the inhibition of cell division and proliferation in tumor cells that overexpress AKs.
T26200 Somatostatin RC 102

Somatostatin RC102,Somatostatin-RC-102,Somatostatin RC-102

Somatostatin RC 102 is a peptide hormone. It regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones.
T68546 PF-00337210

PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may even...
T70152 Miransertib mesylate

Miransertib mesylate is a selective AKT inhibitor that binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may result in reduction in tumor cell proliferation and the induction of tumor cell apoptosis.
T10875 CP5V

Others Others
CP5V, a PROTAC, induces mitotic inhibition, and suppresses cancer cell proliferation. It specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation.
T8082 NSC745887

NSC745887 (compound 25) 是一种抗癌剂, 在所有 60 种癌细胞系中均表现出剂量依赖性的增殖抑制作用。
T70018 Apricoxib

Apricoxib, also known as Benzenesulfonamide 42(4ethoxyphenyl)4methyl1Hpyrrol1yl, is an orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related...
T70198 Atrasentan sodium

Atrasentan, also known as ABT-627, is a orally available ETA receptor antagonist with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.
T71232 Alisertib sodium hydrate

Alisertib sodium hydrate is a salt of Alisertib --- an inhibitor of Aurora A kinase with potential antineoplastic activity. Alisertib binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation.
T81128 Sontigidomide

Sontigidomide(Compound 5)是一种抗肿瘤化合物,能在1 μM浓度下显著抑制MOLM-13细胞增殖,3天内抑制率超过80%。
T60996 SDR-04

SDR-04 对BRD4-BD1 表现出很强的亲和力和抑制活性。SDR-04 是一种BET 抑制剂,可有效抑制 MV4;11 癌细胞系的增殖。
T70808 Cabazitaxel-d6

Cabazitaxel-d6 is a deuterium labeled cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance...
T69305 Milataxel

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) ...
T60479 NSC 698600

NSC 698600 是一种有效的 PCAF(p300/CBP 相关因子)抑制剂,IC50值为 6.51 μM,显示出良好的癌细胞增殖抑制活性。
T70994 TAK-659 HCl

TAK-659 is an inhibitor of spleen tyrosine kinase (syk), with potential anti-inflammatory, immunomodulating, and antineoplastic activities. Spleen tyrosine kinase inhibitor TAK-659 may inhibit the activity of syk, which abrogates downstream B-cell receptor (BCR) signaling and leads to an inhibition of B-cell activation, chemotaxis, adhesion and proliferation. Note: TAK-659 free base is less stable. This product is supplied as dihydrochloride form.
T25716L Liarozole HCl

R75251,Liarozole hydrochloride,R 75251,R-75251

Liarozole HCl is a benzimidazole derivative with antineoplastic activity. As a retinoic acid metabolism blocking agent, liarozole inhibits CYP450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, leading to an increase in endogenous ATRA production,
T69723 Taminadenant mesylate

Taminadenant, also known as PBF-509 and NIR-178, is a potent and orally active adenosine A2A receptor antagonist with potential antineoplastic activity. PBF-509 selectively binds to and inhibits A2AR expressed on T lymphocytes. This abrogates the adenosine/A2AR-mediated inhibition of T-lymphocytes and activates a T-cell-mediated immune response against tumor cells, thereby reducing proliferation of susceptible tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell sur...
T74921 Antiproliferative agent-12

Antiproliferative agent-10 (compound 1) 是一种钌(II)-三吡唑基甲烷抗肿瘤复合物,能够通过阻断线粒体钙吸收来抑制癌细胞增殖。
T70876 KW-2450 Tosylate

KW-2450 Tosylate is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 Tosylate selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in t...
T79782 FPR1 antagonist 2

FPR1 antagonist 2 (compound 25b)为FPR1拮抗剂,IC50值70 nM。该化合物综合影响细胞增殖与凋亡,抑制细胞生长,降低细胞迁移,并促进血管生成。
T79781 FPR1 antagonist 1

FPR1 antagonist 1 (compound 24a)作为一种FPR1拮抗剂,具有25 nM的IC50值。该化合物抑制细胞增殖与凋亡,减少细胞迁移,并诱导血管生成。
T72956 Darizmetinib

HRX215

MAPK MAPK
Darizmetinib (HRX215) 是一种 MKK4 抑制剂,MKK4 的抑制导致 MKK7 和 JNK1 信号通路的增强,进而激活转录因子 ATF2 和 ELK1,促进细胞增殖和肝再生。
T70275 PAT-347

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.
T69985 Lifirafenib HCl

Lifirafenib, also known as Beigene-283, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation/amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the ...
T68760 Luminespib mesylate

Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.

化合物

SKLB4771
Cat.No: T2051
Synonym: FLT3-​IN-​1,FLT3-IN-1
Target: FLT
Roblitinib
Cat.No: T4235
Synonym: FGF-401
Target: FGFR
Etretinate
Cat.No: T6831
Synonym: Retinoid,Tegison,Etretinato,Ethyl etrinoate,Ro 10-9359,依曲替酯
Target: Apoptosis, Others
XL413
Cat.No: T3352
Synonym:
Target: cholecystokinin, Casein Kinase, Pim, CDK
Linsitinib
Cat.No: T6017
Synonym: OSI-906,林西替尼
Target: IGF-1R
Momelotinib
Cat.No: T1849
Synonym: CYT11387,CYT387,LM-1149
Target: Apoptosis, JAK, Autophagy
Cobimetinib
Cat.No: T3623
Synonym: 可美替尼,考比替尼,RG7420,XL518,GDC-0973
Target: Apoptosis, MEK
Icotinib Hydrochloride
Cat.No: T2307
Synonym: 埃克替尼盐酸盐,盐酸埃克替尼,BPI-2009H
Target: EGFR
SAR405
Cat.No: T12831L
Synonym:
Target: PI3K, Autophagy
Etoricoxib
Cat.No: T1574
Synonym: Arcoxia,MK-663,Tauxib,L-791456,Nucoxia,Desvenlafaxine,依托考昔
Target: COX
Midostaurin
Cat.No: T3211
Synonym: 米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱
Target: Others, PKC
Ridaforolimus
Cat.No: T6334
Synonym: AP23573,Deforolimus,MK-8669
Target: mTOR, Autophagy
DRI-C21045
Cat.No: T11096
Synonym:
Target: NF-κB
KW-2450 free base
Cat.No: T68405
Synonym:
Target: IGF-1R
ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate
Cat.No: T50107
Synonym:
Target: Others
Rofecoxib
Cat.No: T1185
Synonym: MK 966,罗非昔布,罗非考昔,MK-0966
Target: COX
Acalabrutinib
Cat.No: T3626
Synonym: ACP-196,阿可替尼
Target: BTK
CBR-5884
Cat.No: T14884
Synonym:
Target: Others, Dehydrogenase
Relugolix
Cat.No: T3630
Synonym: RVT-601,瑞卢戈利,TAK-385
Target: GNRH Receptor
Telomerase-IN-1
Cat.No: T12009
Synonym:
Target: Telomerase
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
BC12
Cat.No: T26752
Synonym: BC 12,BC-12
Target:
SR-31747 free base
Cat.No: T38720
Synonym:
Target:
BMS-243117
Cat.No: T30508
Synonym: UNII-MBE6KWV0QI,CHEMBL67237,MBE6KWV0QI
Target:
YKL-04-085
Cat.No: T29176
Synonym: YKL 04085,YKL04-085,YKL 04-085,YKL-04085
Target:
SNS-314
Cat.No: T21298
Synonym: SNS-314 free base,SNS314,SNS 314
Target:
Somatostatin RC 102
Cat.No: T26200
Synonym: Somatostatin RC102,Somatostatin-RC-102,Somatostatin RC-102
Target:
PF-00337210
Cat.No: T68546
Synonym:
Target:
Miransertib mesylate
Cat.No: T70152
Synonym:
Target:
CP5V
Cat.No: T10875
Synonym:
Target: Others
NSC745887
Cat.No: T8082
Synonym:
Target:
Apricoxib
Cat.No: T70018
Synonym:
Target:
Atrasentan sodium
Cat.No: T70198
Synonym:
Target:
Alisertib sodium hydrate
Cat.No: T71232
Synonym:
Target:
Sontigidomide
Cat.No: T81128
Synonym:
Target:
SDR-04
Cat.No: T60996
Synonym:
Target:
Cabazitaxel-d6
Cat.No: T70808
Synonym:
Target:
Milataxel
Cat.No: T69305
Synonym:
Target:
NSC 698600
Cat.No: T60479
Synonym:
Target:
TAK-659 HCl
Cat.No: T70994
Synonym:
Target:
Liarozole HCl
Cat.No: T25716L
Synonym: R75251,Liarozole hydrochloride,R 75251,R-75251
Target:
Taminadenant mesylate
Cat.No: T69723
Synonym:
Target:
Antiproliferative agent-12
Cat.No: T74921
Synonym:
Target:
KW-2450 Tosylate
Cat.No: T70876
Synonym:
Target:
FPR1 antagonist 2
Cat.No: T79782
Synonym:
Target:
FPR1 antagonist 1
Cat.No: T79781
Synonym:
Target:
Darizmetinib
Cat.No: T72956
Synonym: HRX215
Target: MAPK
PAT-347
Cat.No: T70275
Synonym:
Target:
Lifirafenib HCl
Cat.No: T69985
Synonym:
Target:
Luminespib mesylate
Cat.No: T68760
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5724 Neogambogic acid

neo-gambogic acid,新藤黄酸

Apoptosis; Others; Antibacterial Apoptosis; Microbiology/Virology; Others
Neogambogic acid 是藤黄的有效成分,可诱导细胞凋亡并具有抗癌作用。它有效抑制耐甲氧西林的金黄色葡萄球菌。
TN1516 Cnidicin

蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮

NOS; NO Synthase Immunology/Inflammation
Cnidicin 是一种香豆素,对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。
T3877 Esculentoside A

NF-κB; COX Immunology/Inflammation; Neuroscience; NF-κB
Esculentoside A 是一种三萜皂苷,从商陆根部分离得到。它在具有抗炎活性,对环氧合酶-2 具有选择性抑制活性。它通过抑制NF-κB 和丝裂原活化蛋白激酶信号通路抑制 LPS 诱导的急性肺损伤中的炎症反应。
T5S0527 Rhodojaponin III

闹羊花素 Ⅲ,闹羊花毒素III

Others Others
Rhodojaponin III 是二萜类化合物,提取于Rhododendron molle 叶子,具有抗炎作用。
T6S1141 Ganoderic acid A

灵芝酸 A,灵芝酸A

Apoptosis; NF-κB; Endogenous Metabolite; Autophagy Apoptosis; Autophagy; Metabolism; NF-κB
Ganoderic acid A 能够抑制 JAK-STAT3信号通路,也能抑制细胞增殖,存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。
T3S0153 Xanthatin

苍耳亭,叶黄制菌素

Apoptosis; VEGFR; Lipoxygenase; Wnt/beta-catenin; Antibacterial Angiogenesis; Apoptosis; Cytoskeletal Signaling; Metabolism; Microbiology/Virology; Stem Cells; Tyrosine Kinase/Adaptors
Xanthatin 是一种从Xanthium strumarium 叶子中提取的天然产物,可诱导细胞凋亡。它抑制布鲁氏菌的IC50值为 2.63 μg/ mL,对寄生虫特异性锥虫硫磷还原酶具有不可逆的弱抑制作用。它通过抑制PGE2的合成和 5-脂氧合酶的活性而显示出抗炎活性。
T3229 Cytochalasin D

ATPase; p38 MAPK; Calcium Channel; Akt; PI3K Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
T6S1917 Schisandrol B

Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

P450; Reactive Oxygen Species; Autophagy Autophagy; Immunology/Inflammation; Metabolism; NF-κB
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。
T2836 Isorhamnetin

3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin

MEK; PI3K; Endogenous Metabolite MAPK; Metabolism; PI3K/Akt/mTOR signaling
Isorhamnetin (3-methylquercetin) 是从中草药沙棘中提取的一种类黄酮,可通过抑制MEK1和PI3K 来抑制皮肤癌。
TN3972 Epimedokoreanin B

Apoptosis; Others; Antibacterial Apoptosis; Microbiology/Virology; Others
Epimedokoreanin B (EKB) 是一种从韩国淫羊藿中分离出的异戊烯化类黄酮,在人非小细胞肺癌(NSCLC)A549和NCI-H292细胞中展现出抗癌活性。Epimedokoreanin B 还具有抗炎和抗菌活性,可有清除 DPPH 自由基的活性,能以剂量依赖的方式抑制 MCF-7 和 HepG2 的增殖。Epimedokoreanin B 能显著抑制 N (δ) -(羧甲基)赖氨酸(CML)和 N (Ï) -(羧甲基)精氨酸(CMA)的形成,可通过抑制高级糖化终产物(AGEs)预防糖尿病的临床并发症。
T11363 Ganoderic acid F

Others Others
Ganoderic acid F 是一种灵芝酸。它具有抗肿瘤和抗转移的活性,与抑制血管生成和涉及细胞增殖和细胞死亡,致癌作用,氧化应激,钙信号传导和内质网应激的蛋白质改变等机制相关。
TN6586 12-Oleanene-3,6-diol

12-Oleanene-3,6-diol has antitumor activity, it can induce apoptosis and has inhibition effect on the proliferation in RKO cell line.
TN4239 Hydroxytanshinone IIA

Others Others
Hydroxytanshinone ⅡA has good antiproliferative effect on SGC-7901,HeLa, and HepG 2 cell, the values of IC50 are 4.18, 6.08 and10.20 uM, respectively; it has tumor cell proliferation inhibition significantly stronger than the tanshinoneⅡA.
TN1428 (+)-Balanophonin

Antioxidant; AChE Neuroscience; oxidation-reduction
(+)-Balanophonin 是一种从 Passiflora edulis 分离得到的天然酚类化合物,具有抗氧化、抗炎、抗癌和抗神经退行性活性,抑制胆碱酯酶,对 OPM2 和 RPMI-8226 细胞增殖有边际抑制作用。
T70495 Scytonemin

Scytonemin is a biological pigment synthesized by many strains of cyanobacteria, including Calothrix sp., Lyngbya aestuarii, and others. Scytonemin is also a potent PKL1 inhibitor, which inhibits cell proliferation and arrests cell cycle through downregulating Plk1 activity in many cancel cells. Scytonemin was able to inhibit the proliferation of three myeloma cells in a dose-dependent manner, while U266 was the most sensitive one to scytonemin. Scytonemin , representing a novel Plk1 inhibitor, ...
T75704 Isoharringtonine

Isoharringtonine,一种从Cephalotaxus koreanaNakai 纯化得到的天然生物碱,具有抑制癌细胞增殖和迁移的能力,同时能诱导癌细胞(apoptosis)。该化合物在癌症研究中应用。
TN4490 Manassantin B

ERK; BCL; p38 MAPK; TNF; NF-κB; JNK; STAT; Antifection Apoptosis; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells
Manassantin B is a potent inhibitor of NF-κB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-κB. It also possesses anti-EBV lytic replication activity. Manassantin B inhibits interleukin-6-induced signal transducer and activator of transcription 3 activation in Hep3B cells, it has potential as a potent anti-inflammatory drug for use in pathological processes such as sepsis or acute lung injury. Manassantin B exerts antifibrotic activity in HSC-T6 cells, in pa...
TN3364 Agrimonolide

Apoptosis; Dehydrogenase; p38 MAPK; ROS; JAK Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; MAPK; Metabolism; Stem Cells
Agrimonolide 是一种来自异香豆素的化合物,主要存在于草药Agrimonia pilosa Ledeb 中,具有显著的生物活性。Agrimonolide 通过抑制脂多糖(LPS)诱导的JAK-STATs 和p38 MAPKs 信号通路的激活而发挥抗炎作用。Agrimonolide 及其衍生物去甲阿戈莫内德已显示出能够有效提高肝细胞中胰岛素介导的糖原水平,可能在调节胰岛素抵抗的HepG2细胞中发挥关键作用。Agrimonolide 通过靶向卵巢癌细胞中的SCD1,对癌症的进展和诱导细胞死亡和凋亡表现出抑制作用。特别是,Agrimonolide 对A2780和SKOV-3细胞的增殖、迁移和侵袭表现出剂量依赖性的抑制,同时促进细胞凋亡。该化合物还被发现能诱导铁介导的细胞死亡,同时增加活性氧(ROS)和总铁的水平。Agrimonolide 很容易穿过血脑屏障,表明其在神经系统疾病的治疗应用方面具有潜力。

天然产物

Neogambogic acid
Cat.No: T5724
Synonym: neo-gambogic acid,新藤黄酸
Target: Apoptosis, Others, Antibacterial
Cnidicin
Cat.No: TN1516
Synonym: 蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮
Target: NOS, NO Synthase
Esculentoside A
Cat.No: T3877
Synonym:
Target: NF-κB, COX
Rhodojaponin III
Cat.No: T5S0527
Synonym: 闹羊花素 Ⅲ,闹羊花毒素III
Target: Others
Ganoderic acid A
Cat.No: T6S1141
Synonym: 灵芝酸 A,灵芝酸A
Target: Apoptosis, NF-κB, Endogenous Metabolite, Autophagy
Xanthatin
Cat.No: T3S0153
Synonym: 苍耳亭,叶黄制菌素
Target: Apoptosis, VEGFR, Lipoxygenase, Wnt/beta-catenin, Antibacterial
Cytochalasin D
Cat.No: T3229
Synonym:
Target: ATPase, p38 MAPK, Calcium Channel, Akt, PI3K
Schisandrol B
Cat.No: T6S1917
Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B
Target: P450, Reactive Oxygen Species, Autophagy
Isorhamnetin
Cat.No: T2836
Synonym: 3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin
Target: MEK, PI3K, Endogenous Metabolite
Epimedokoreanin B
Cat.No: TN3972
Synonym:
Target: Apoptosis, Others, Antibacterial
Ganoderic acid F
Cat.No: T11363
Synonym:
Target: Others
12-Oleanene-3,6-diol
Cat.No: TN6586
Synonym:
Target:
Hydroxytanshinone IIA
Cat.No: TN4239
Synonym:
Target: Others
(+)-Balanophonin
Cat.No: TN1428
Synonym:
Target: Antioxidant, AChE
Scytonemin
Cat.No: T70495
Synonym:
Target:
Isoharringtonine
Cat.No: T75704
Synonym:
Target:
Manassantin B
Cat.No: TN4490
Synonym:
Target: ERK, BCL, p38 MAPK, TNF, NF-κB, JNK, STAT, Antifection
Agrimonolide
Cat.No: TN3364
Synonym:
Target: Apoptosis, Dehydrogenase, p38 MAPK, ROS, JAK
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