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抑制剂 & 化合物

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。
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 ...

化合物

Regorafenib monohydrate

Cat.No: T1792L

Synonym:

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

Regorafenib

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

PHD-IN-1

Cat.No: T79797

Synonym:

Target: HIF/HIF Prolyl-Hydroxylase

Menin-MLL inhibitor 29

Cat.No: T79737

Synonym:

Target: Epigenetic Reader Domain

Cat. No.	Product Name	Target	Signaling Pathways
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。
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...