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35

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T2298	ML204	TRP/TRPV Channel	Membrane transporter/Ion channel
	ML204 是有效的TRPC4/TRPC5通道选择性抑制剂，相比于 TRPC6 ，对TRPC4/TRPC5通道的选择性高出 19 倍，不影响其他的 TRP 通道和电压门控的钠、钾或 Ca2+通道。
T15633	JW74	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	JW74 能够拮抗 LiCl 诱导的经典 Wnt 信号激活 (IC50: 420 nM)。
T7399	LF3	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	LF3 是一种典型 Wnt 信号传导的特异性抑制剂，通过破坏 β-catenin 和 TCF4 之间的相互作用（IC50 < 2 μM）
T22884	JW 67	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	JW 67 是典型 Wnt 信号通路的抑制剂，IC50为 1.17 μM。它影响由 β- 连环蛋白/GSK-3β/AXIN/APC/CK1 组成的多蛋白复合物，快速降低活性 β- 连环蛋白，随后下调Wnt 靶基因。它也抑制结直肠癌细胞生长。
T16687	Pyr3	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr3 是一种选择性瞬时受体电位经典通道 3 抑制剂。 Pyr3 以剂量依赖性方式抑制 TRPC3 介导的 Ca2+ 内流 (IC50 = 700 nM)。
T4662	SJ000291942	TGF-beta/Smad	Stem Cells
	SJ000291942 是一种经典骨形态发生蛋白 (BMP) 信号传导途径的激活剂。其中 BMP 是一种转化生长因子 β 分泌信号分子家族的成员。
T8820	BML-284 hydrochloride BML-284 HCL,Wnt agonist 1 HCL	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	BML-284 hydrochloride (Wnt agonist 1 HCL) 是细胞通透性 Wnt 信号激活剂。它能够诱导 TCF 依赖的转录活性(EC50>700 nM)。
T9263	cim0216 N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	CIM0216 是选择性的TRPM3激动剂，对 TRPM3 的选择性高于 TRPM1、TRPM2 和 TRPM4-8。它以TRPM3依赖性的方式引起疼痛并唤起感觉神经末梢的神经肽释放，可用于神经源性炎症的相关研究。
T8404	Kasugamycin hydrochloride hydrate Ksg (hydrochloride hydrate),春雷霉素盐酸盐一水合物	Antibacterial; Antibiotic	Microbiology/Virology
	Kasugamycin hydrochloride hydrate (Ksg (hydrochloride hydrate)) 是一种能结合 30s 和 70s 核糖体，但不能结合 50s 亚基的抗生素。它模拟 mRNA 核苷酸破坏 tRNA 结合并抑制典型翻译起始。
T3701	MCC950 CP-456773	NOD	Immunology/Inflammation; NF-κB
	MCC950 (CP-456773) 是NLRP3的选择性抑制剂，能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。
T12797	RU-SKI 43 RUSKI 43	Hedgehog/Smoothened; Acyltransferase	GPCR/G Protein; Metabolism; Stem Cells
	RU-SKI 43 是一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850 nM。RU-SKI 43 具有抗癌活性，是治疗肺腺癌的潜在化合物。RU-SKI 43 通过独立于平滑化的非规范信号传导降低 Gli-1 激活，并抑制 Akt 和 mTOR 通路活性。
T13213	TRPC6-IN-1	Others	Others
	TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).
T34271	RBPI-3
	RBPI-3 is a canonical poly(ADP-ribose) glycohydrolase.
T69842	DB2313 HCl
	DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.
T72008	E09241
	E09241 is a novel OPG/RANKL upregulator, increasing OPG expression without affecting RANKL expression, promoting osteoblast differentiation while inhibiting osteoclast differentiation, regulating OPG expression through canonical Wnt/β-catenin signaling.
T18864	UAA crosslinker 1	Others	Others
	UAA crosslinker 1 hydrochloride is an Amber codon-activating agent utilized for the incorporation of non-canonical amino acids (ncAAs) into proteins. This incorporation is achieved in vivo by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].
T71147	PBS-1086
	PBS-1086 is a novel dual inhibitor of the canonical and noncanonical NF-κB pathways, increasing the magnitude and duration of initial EGFR inhibitor response in multiple NSCLC models, decreasing PDHK1 expression, and suppressing phosphorylation of the PDHK1 protein substrate PDHA1 in a panel of PTEN-deficient cell lines.
T60357	NF-κB-IN-2 JEUD-38
	NF-κB-IN-2 抑制 PC-3细胞中 TNF-α诱导的的经典 NF-κB 信号传导。
T69771	MS-177
	MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
T18863	UAA crosslinker 1 hydrochloride	Others	Others
	UAA crosslinker 1 hydrochloride is an amber codon used to incorporate non-canonical amino acids (ncAAs) into proteins in vivo. This is achieved by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].
T60365	SY-LB-35
	SY-LB-35 是骨形态发生蛋白 (BMP) 受体的有效激动剂。SY-LB-35 可以刺激 C2C12 成肌细胞系中细胞数量和细胞活力的显著增加，并引起细胞周期向 S 期和 G2/M 期转变。SY-LB-35 刺激典型的 Smad 和非典型的 PI3K/Akt、ERK、p38和 JNK 胞内信号通路。
T75550	Hyp9
	Hyp9为特异性激动剂，针对瞬时受体电位阳离子通道6（TRPC6），应用于脊髓损伤（SCI）的研究。
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.
T61407	TRPC3/6-IN-1
	TRPC3/6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3/6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1].
T78120	β-catenin-IN-6
	β-catenin-IN-6是一种针对Wnt/β-catenin(典型的wingless相关整合位点)通路的抑制剂，能够抑制人类结直肠癌细胞的增殖，并在β-catenin/RK3E小鼠模型上展现出效果。
T38091	3'3'-cGAMP (sodium salt)
	3'3'-cGAMP is a second messenger produced in bacteria by specific dinucleotide cyclases. It contains canonical 3'5'-phosphodiester bonds and regulates chemotaxis, colonization, and other cellular functions. 3'3'-cGAMP shows weaker binding to the adapter protein stimulator of interferon genes (STING; Kd = 1.04 μM) than 2'2'-cGAMP and 2'3'-cGAMP but has similar binding affinity to 3'2'-cGAMP (Kd = 1.61 μM) and cyclic di-GMP . 3'3'-cGAMP induces IFN-β mRNA expression in L929 cells (EC50 = 40.5 nM).
TP1565L	Foxy-5 acetate Foxy-5 acetate(881188-51-8 free base)	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Foxy-5 acetate 是 Wnt 5A 的激动剂，Wnt 5A 是 Wnt 家族的非经典成员。 Foxy-5 acetate 损害上皮癌细胞的迁移和侵袭，触发细胞溶质游离钙信号传导，而不影响 β-连环蛋白活化。
T79638	Lepadin E	Glutathione Peroxidase	Metabolism
	Lepadin E 是一种铁死亡（ferroptosis）诱导剂，它通过激活 p53-SLC7A11-GPX4 途径显著诱发细胞毒性。该化合物增强 p53 的表达，减少 SLC7A11 及 GPX4 的水平，进而导致活性氧 (ROS) 和脂质过氧化物的增加，并通过上调 ACSL4 来促进细胞死亡。Lepadin E 还具有显著的抗肿瘤效果。
T38303	Apramycin (Nebramycin II)
	Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A bas...
T35654	2'2'-cGAMP (sodium salt)
	2'2'-cGAMP is a synthetic dinucleotide (CDN) that contains non-canonical 2'5'-phosphodiester bonds. It binds to the adapter protein stimulator of interferon genes , which is a component of the innate immune response that activates the type I interferon pathway when bound to cyclic dinucleotides. 2'2-cGAMP shows weaker binding to STING than 2'3'-cGAMP but binds more strongly than 3'3'-cGAMP , cyclic di-GMP , or 3'2'-cGAMP, which bind in the micromolar range (Kds = 1.04, 1.21, or 1.61 μM, respecti...
T75941	Foxy-5 TFA
	Foxy-5 TFA 是WNT5A 激动剂，是 WNT5A 的一个模拟肽，是Wnt 家族的非经典成员。Foxy-5 TFA 可在不影响β-catenin 激活的情况下触发胞浆游离钙信号传导，并可抑制上皮癌细胞的迁移和侵袭。Foxy-5 TFA 在原位小鼠模型中能有效降低 WNT5A 低表达的前列腺癌细胞的转移扩散。
T71303	Flufenamic Acid-d4
	Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...
T36995	MRT 68601 hydrochloride
	Potent TBK1 (TANK-binding kinase-1) inhibitor (IC50 = 6 nM). Inhibits the formation of autophagosomes in lung cancer cells. Newman et al (2012) TBK1 kinase addiction in lung cancer cells is mediated via autophagy of Tax1bp1/Ndp52 and non-canonical NF-κB signalling. PLoS ONE 7 e50672 PMID:23209807 \|McIver et al (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. Bioorg.Med.Chem.Lett. 22 7169 PMID:23099093
T37763	BTD
	Selective TRPC5 activator (EC50 = 1.4 μM in a calcium influx assay, 1.3 μM in whole cell patch clamp assay). Displays >14.5-fold selectivity for TRPC5 over other TRP channels (EC50 = 20.6 μM for TRPM8). Also activates TRPC1:5 and TRPC4:5 heteromers. Beckmann et al (2017) A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels. Cell Calcium. 66 10 PMID:28807145
T36616	DTUN
	DTUN is a lipophilic hyponitrite radical initiator.1It initiates co-autoxidation of STY-BODIPY-embedded egg phosphatidylcholine liposomes when used at a concentration of 0.2 mM. DTUN has been used in fluorescence-enabled inhibited autoxidation (FENIX) assays for the development of ferroptosis inhibitors and the study of antioxidants in lipid membranes.1,2 1.Shah, R., Farmer, L.A., Zilka, O., et al.Beyond DPPH: Use of fluorescence-enabled inhibited autoxidation to predict oxidative cell death res...

化合物

Cat.No: T2298

Target: TRP/TRPV Channel

Cat.No: T15633

Target: Wnt/beta-catenin

Cat.No: T7399

Target: Wnt/beta-catenin

Cat.No: T22884

Target: Wnt/beta-catenin

Cat.No: T16687

Target: TRP/TRPV Channel

Cat.No: T4662

Target: TGF-beta/Smad

BML-284 hydrochloride

Cat.No: T8820

Synonym: BML-284 HCL,Wnt agonist 1 HCL

Target: Wnt/beta-catenin

Cat.No: T9263

Synonym: N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide

Target: TRP/TRPV Channel

Kasugamycin hydrochloride hydrate

Cat.No: T8404

Synonym: Ksg (hydrochloride hydrate),春雷霉素盐酸盐一水合物

Target: Antibacterial, Antibiotic

Cat.No: T3701

Synonym: CP-456773

Target: NOD

Cat.No: T12797

Synonym: RUSKI 43

Target: Hedgehog/Smoothened, Acyltransferase

Cat.No: T13213

Target: Others

Cat.No: T34271

Cat.No: T69842

Cat.No: T72008

UAA crosslinker 1

Cat.No: T18864

Target: Others

Cat.No: T71147

Cat.No: T60357

Synonym: JEUD-38

Cat.No: T69771

UAA crosslinker 1 hydrochloride

Cat.No: T18863

Target: Others

Cat.No: T60365

Cat.No: T75550

β-catenin-IN-37

Cat.No: T39200

Cat.No: T61407

β-catenin-IN-6

Cat.No: T78120

3'3'-cGAMP (sodium salt)

Cat.No: T38091

Cat.No: TP1565L

Synonym: Foxy-5 acetate(881188-51-8 free base)

Target: Wnt/beta-catenin

Cat.No: T79638

Target: Glutathione Peroxidase

Apramycin (Nebramycin II)

Cat.No: T38303

2'2'-cGAMP (sodium salt)

Cat.No: T35654

Cat.No: T75941

Flufenamic Acid-d4

Cat.No: T71303

MRT 68601 hydrochloride

Cat.No: T36995

Cat.No: T37763

Cat.No: T36616

Cat. No.	Product Name	Target	Signaling Pathways
TN7036	N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide,间-甲氧基苄基-亚麻酰胺,Macamide Impurity 14	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (Macamide Impurity 14) 是一种从玛卡中分离得到的玛卡酰胺。它能够激活典型的Wnt/β‐catenin 信号通路，诱导间充质干细胞成骨分化和随后的骨形成，可用于研究骨质疏松症。
T15541	Hyperforin dicyclohexylammonium salt Hyperforin DCHA	Others	Others
	Hyperforin dicyclohexylammonium salt is a transient receptor canonical 6 channel activator with antidepressant effect. It modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels.

天然产物

N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide

Cat.No: TN7036

Synonym: (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide,间-甲氧基苄基-亚麻酰胺,Macamide Impurity 14

Target: Wnt/beta-catenin

Hyperforin dicyclohexylammonium salt

Cat.No: T15541

Synonym: Hyperforin DCHA

Target: Others

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