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22

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T1792L	Regorafenib monohydrate	Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy	Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors
	Regorafenib monohydrate 是一种新型口服多激酶抑制剂，对VEGFR1/2/3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。
T22443	Triglycidyl isocyanurate Tris(2,3-epoxypropyl) Isocyanurate,Teroxirone,TGIC,1,3,5-三缩水甘油-S-三嗪三酮,TGI	Apoptosis	Apoptosis
	Triglycidyl isocyanurate (Teroxirone) 是一种三氮烯三环氧化合物，可通过 p53的激活抑制非小细胞肺癌细胞的生长。它诱导细胞凋亡，具有抗血管生成和抗肿瘤活性，用于癌症研究。
T1792	Regorafenib BAY 73-4506,瑞戈非尼,Fluoro-Sorafenib,瑞格非尼	Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy	Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors
	Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5/2.5/4.2/7/13/22 nM)，具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。
T12372	PAT-505	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	PAT-505 是一种可口服且具有选择性和高效性的自体表皮生长因子抑制剂（在 Hep3B 细胞中的 IC50 为 2 nM，在人体血液中的 IC50 为 9.7 nM，在小鼠血浆中的 IC50 为 62 nM）。
T15109	DGAT1-IN-1	Transferase	Metabolism
	DGAT1-IN-1是 DGAT1的高效抑制剂，在 Hep3B 细胞过表达 DGAT1裂解物中，测得IC50低于10nM。
T80632	Methyl 3,4-dimethoxycinnamate
	Methyl 3,4-dimethoxycinnamate 组成中展现出对黑孢子萌发的抑制作用，并且在 Hep3B 细胞中抑制整体 DNA 甲基化。
T74371	LEB-03-146
	LEB-03-146是一种WEE1DUBTAC（去泛素化酶靶向嵌合体），通过PEG2连接剂把AZD1775 (Adavosertib) 和OTUB1招募者EN523相连。在HEP3B肝癌细胞中，LEB-03-146能显著增强WEE1的稳定性。
T79797	PHD-IN-1	HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; Metabolism
	PHD-IN-1（compound 80）作为PHD2的抑制剂，显示出 IC50 ≤5 nM 的高效活性。在Caco2-HIFla-HiBiT-clone-1和Hep3B细胞系中进行的EPO Elisa实验中，其EC50值均为2.5 μM。
T74275	LEB-03-144
	LEB-03-144 是一个 WEE1DUBTAC (去泛素化酶靶向嵌合体)，通过 C3 烷基连接剂将 AZD1775 (Adavosertib) 与 OTUB1招募者 EN523 连接起来。LEB-03-144 在 HEP3B 肝癌细胞中可显著稳定WEE1。
T79798	PHD-IN-2	HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; Metabolism
	PHD-IN-2（Compound 91）是一种高效的PHD拮抗剂，具有IC50值小于5 nM，能在HEP3B细胞中诱导促红细胞生成素的合成，EC50值小于2.5 μM。此化合物主要用于心血管、代谢、血液、肺部、肾脏、肝脏疾病、伤口愈合以及癌症等研究领域。
T69966	Roxadustat-d5
	Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and ...
T40112	PROTAC PD-1/PD-L1 degrader-1 PROTAC PD-1/PD-L1 degrader-1
	PROTAC PD-1/PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1/PD-L1 PROTAC that effectively inhibits the interaction between PD-1 and PD-L1 with an IC50 value of 39.2 nM. It successfully restores the suppressed immune response in a co-culture model consisting of Hep3B/OS-8/hPD-L1 cells and CD3 T cells. Additionally, this compound moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.
T35690	Myceliothermophin E
	Myceliothermophin E is a polyketide-amino acid hybrid fungal metabolite that has been found inT. thermophilusand has anticancer and antimicrobial activities.1,2It is cytotoxic to DLD-1, Hep3B, HepG2, and HGC-27 cancer cells (IC50s = 0.32, 0.42, 0.26, and 0.08 μg/ml, respectively).1Myceliothermophin E is active against methicillin-resistant, but not -sensitive,S. aureus(MICs = 15.8 and >100 μM, respectively).2 1.Gao, Y.-L., Zhang, M.-L., Wang, X., et al.Isolation and characterization of a new cyt...
T73121	FGFR4-IN-8	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	FGFR4-IN-8 (Compound 7v) 是 ATP 竞争性、高选择性的 FGFR4 野生型及其突变体共价抑制剂，对 FGFR4、FGFR4V550L、FGFR4V550M 及 FGFR4C552S 的 IC50 值分别为 0.5、0.25、1.6、931 nM。该化合物能有效抑制 Hep3B 肝细胞癌细胞增殖，显示出显著的抑制效果，具有潜在的临床应用价值。
T61968	PD-1/PD-L1-IN 6
	PD-1/PD-L1-IN 6 (compound A13) 是有效的PD-1/PD-L1相互作用抑制剂（IC50为 132.8 nM）。PD-1/PD-L1-IN 6 显示出显著的免疫调节活性。在 Hep3B/OS-8/hPD-L1 与 CD3 T 细胞共培养模型中，PD-1/PD-L1-IN 6显著提高干扰素 -γ 分泌，且无明显毒性作用。在 T 细胞-肿瘤共培养模型中，PD-1/PD-L1-IN 6恢复免疫应答。
T79737	Menin-MLL inhibitor 29	Epigenetic Reader Domain	Chromatin/Epigenetic
	Menin-MLL inhibitor 29（Compound C1）是一种选择性Menin-MLLPPI抑制剂。该化合物与Menin紧密结合，具有138 nM的KD值，并以46 nM的IC50值明显抑制Menin与MBM1（Menin结合motif 1）的相互作用。在体外条件下，Menin-MLL inhibitor 29对HepG2和Hep3B肝癌细胞系表现出抑制增殖的作用（IC50s分别为0.31 μM和0.71 μM），也能有效抑制肿瘤生长。
T35771	Destruxin B2
	Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 ...
T36713	Streptochlorin
	Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio...
T6345	Tirbanibulin KX2-391,KX-01	Microtubule Associated; Src	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Tirbanibulin (KX2-391) 是一种高度选择性的 Src 激酶抑制，靶向 Src 的多肽底物结合位点，对多种癌症有疗效。
T15675	Tirbanibulin Mesylate KX2-391 Mesylate,KX01 Mesylate	Microtubule Associated; Src	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Tirbanibulin Mesylate (KX01 Mesylate) 是一种 Src 抑制剂，靶向 Src 的肽底物位点。在肿瘤细胞中，GI50值为 9-60 nM。
T15674	Tirbanibulin dihydrochloride KX-01 (dihydrochloride),KX2-391 (dihydrochloride)	Src	Angiogenesis; Tyrosine Kinase/Adaptors
	Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).

化合物

Cat.No: T4235

Synonym: FGF-401

Target: FGFR

Regorafenib monohydrate

Cat.No: T1792L

Target: Raf, VEGFR, c-RET, PDGFR, c-Kit, Autophagy

Triglycidyl isocyanurate

Cat.No: T22443

Synonym: Tris(2,3-epoxypropyl) Isocyanurate,Teroxirone,TGIC,1,3,5-三缩水甘油-S-三嗪三酮,TGI

Target: Apoptosis

Cat.No: T1792

Synonym: BAY 73-4506,瑞戈非尼,Fluoro-Sorafenib,瑞格非尼

Target: Raf, VEGFR, c-RET, PDGFR, c-Kit, Autophagy

Cat.No: T12372

Target: EGFR

Cat.No: T15109

Target: Transferase

Methyl 3,4-dimethoxycinnamate

Cat.No: T80632

Cat.No: T74371

Cat.No: T79797

Target: HIF/HIF Prolyl-Hydroxylase

Cat.No: T74275

Cat.No: T79798

Target: HIF/HIF Prolyl-Hydroxylase

Cat.No: T69966

PROTAC PD-1/PD-L1 degrader-1

Cat.No: T40112

Synonym: PROTAC PD-1/PD-L1 degrader-1

Myceliothermophin E

Cat.No: T35690

Cat.No: T73121

Target: FGFR

PD-1/PD-L1-IN 6

Cat.No: T61968

Menin-MLL inhibitor 29

Cat.No: T79737

Target: Epigenetic Reader Domain

Cat.No: T35771

Cat.No: T36713

Cat.No: T6345

Synonym: KX2-391,KX-01

Target: Microtubule Associated, Src

Tirbanibulin Mesylate

Cat.No: T15675

Synonym: KX2-391 Mesylate,KX01 Mesylate

Target: Microtubule Associated, Src

Tirbanibulin dihydrochloride

Cat.No: T15674

Synonym: KX-01 (dihydrochloride),KX2-391 (dihydrochloride)

Target: Src

Cat. No.	Product Name	Target	Signaling Pathways
T3673	Mollugin 大叶茜草素,Rubimaillin	HER; JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Mollugin (Rubimaillin) 是Rubia cordifolia L.中主要的生物活性成分。它能通过 p38-Smad 信号通路增强 BMP-2 的成骨作用。它通过抑制 TNF-α 诱导的 NF-κB 激活起抗癌疗效。
T4S0145	Corylifol A Corylinin,补骨脂异黄酮A	hCE; STAT; UGT	JAK/STAT signaling; Metabolism; Stem Cells
	Corylifol A (Corylinin) 是补骨脂中的一种天然产物，可抑制IL-6 诱导的STAT3激活和磷酸化，IC50值为0.81 μM。
T4964	steviolbioside CCRIS-6025,菊双糖甙,甜菊双糖苷	Others	Others
	Steviolbioside (CCRIS-6025) 是一种存在于甜菊叶中的罕见甜味剂。它对几种人类癌细胞有抑制作用，对乳腺癌具有潜在的研究价值。
T3795	Corilagin	Apoptosis; TLR; Reverse Transcriptase; Antibacterial; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology
	Corilagin 是一种鞣酸，有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长，MIC 为 25 μg/mL。它有抗肿瘤活性，可用于肝癌和卵巢癌。
TN2417	Furomollugin 5-羟基萘并[1,2-B]呋喃-4-甲酸甲酯,呋喃大叶茜草素	Antifection	Microbiology/Virology
	Furomollugin has antiviral activity, it can strongly suppress the secretion of hepatitis B surface antigen (HBsAg), with IC50 = 2.0 micrograms/mL, in human hepatoma Hep3B cells.
T72509	Apoptosis inducer 5
	Apoptosisinducer 5 是一种木脂素对映异构体，存在于Crataegus pinnatifida 中。Apoptosisinducer 5 通过 Hep3B 细胞中的凋亡和自噬表现出细胞毒性作用。
T80942	Triptonoditerpenic acid
	Triptonoditerpenic acid 为一芳香族松香烷二萜类化合物，源自Tripterygium wilfordii。该化合物对HepG2、Hep3B 及 Bcap37细胞株展现细胞毒性作用，其IC50值依次为42.53 μM、29.74 μM 与37.63 μM。
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.
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-ÎºB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-ÎºB. 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...

天然产物

Cat.No: T3673

Synonym: 大叶茜草素,Rubimaillin

Target: HER, JAK

Cat.No: T4S0145

Synonym: Corylinin,补骨脂异黄酮A

Target: hCE, STAT, UGT

Cat.No: T4964

Synonym: CCRIS-6025,菊双糖甙,甜菊双糖苷

Target: Others

Cat.No: T3795

Target: Apoptosis, TLR, Reverse Transcriptase, Antibacterial, Autophagy

Cat.No: TN2417

Synonym: 5-羟基萘并[1,2-B]呋喃-4-甲酸甲酯,呋喃大叶茜草素

Target: Antifection

Apoptosis inducer 5

Cat.No: T72509

Triptonoditerpenic acid

Cat.No: T80942

2,3,24-Trihydroxy-12-ursen-28-oic acid

Cat.No: TN2685

Target: Antifection

Cat.No: TN4490

Target: ERK, BCL, p38 MAPK, TNF, NF-κB, JNK, STAT, Antifection

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