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30

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11394	GFB-8438	TRP/TRPV Channel	Membrane transporter/Ion channel
	GFB-8438 是有效的TRPC5选择性抑制剂，对 hTRPC5 和 hTRPC4 的IC50分别为 0.18 和 0.29 μM。它对 TRPC6、其他 TRP 家族成员、NaV1.5 具有良好的选择性，对 hERG 通道的活性也有限。它对小鼠足细胞的保护作用。
T23312	SB 204741	5-HT Receptor	GPCR/G Protein; Neuroscience
	SB 204741 是一种选择性的5-HT2B 拮抗剂，具有高亲和性，pKi 值为7.1。
T9765	TJ-M2010-5	MyD88	Immunology/Inflammation
	TJ-M2010-5 是一种 MyD88 抑制剂，可与 TIR 结构域结合以干扰其同源二聚化并抑制 MyD88 信号传导。 TJ-M2010-5 可用于心肌缺血/再灌注损伤研究。
T15418	GS-6201 CVT-6883	Adenosine Receptor	GPCR/G Protein; Neuroscience
	GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。
T5443	JQ-1 (carboxylic acid) JQ-1 carboxylic acid	Epigenetic Reader Domain	Chromatin/Epigenetic
	JQ-1 (carboxylic acid) 是一种细胞渗透性 BRD4 抑制剂，对 BRD4(1) 和 BRD4(2) 的 IC50 分别为 77 和 33 nM。它是一种 (+)-JQ1 衍生物，可作为合成 PROTACs 的前体。
T24115	GSK854 GSK-854,GSK 854	Apoptosis	Apoptosis
	GSK854 是一种具有高选择性和有效性的肌钙蛋白 I 相互作用激酶 (TNNI3K) 抑制剂，抑制小鼠心肌梗死损伤细胞焦亡和细胞凋亡，可限制缺血性心脏的氧化应激、损伤和不良重塑。
T9566	PY-60	Annexin A; YAP	GPCR/G Protein; Stem Cells
	PY-60 有效激活针对膜联蛋白 A2 (Kd = 1.4 µM) 的 YAP 转录活性。 PY-60 在能够通过增殖重塑表皮的成年动物中激活促增殖、依赖于 YAP 的转录程序。
T13360	XRK3F2	Autophagy	Autophagy
	XRK3F2 是 p62-ZZ 结构域的抑制剂，在体外减弱 MM 诱导的 Runx2 抑制，在体内肿瘤存在的情况下诱导新骨形成和重塑。
T77617	MMP-9-IN-6	MMP	Proteases/Proteasome
	MMP-9-IN-6 是一种 MMP-9 抑制剂，其 IC50 值为50 μM, 具有较好的抗溃疡功效。MMP-9-IN-6 具有潜在的抗肿瘤活性，可用于研究组织重塑、伤口修复和动脉粥样硬化。
T2129	Zaprinast	PDE	Metabolism
	Zaprinast 是一种 cGMP 选择性的磷酸二酯酶(PDE)抑制剂，是一种 GPR35激动剂，对大鼠 GPR35 有很强的激活作用，对人 GPR35 有一定的激活作用。它通过抗增殖和促凋亡作用，减少血管的重构。
T12721	Rho-Kinase-IN-1	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Rho-Kinase-IN-1 是一种 ROCK 抑制剂，对 ROCK1 和 ROCK2 的 Kis 分别为 30.5 nM 和 3.9 nM。 Rho-Kinase-IN-1 可用于细胞过度增殖、重塑、水肿和炎症疾病的研究。
T21632	Myoseverin	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	Myoseverina 是多核肌管可逆分裂成单核片段的诱导剂，影响多种生长因子、免疫调节、细胞外基质重塑和应激反应基因的表达，与伤口愈合和组织再生相关通路的激活一致。
T3661	Citarinostat ACY241,HDAC-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂，具有抗肿瘤活性，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。
T3712	Mivebresib ABBV-075,米维布塞	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂，结合BRD4的Ki 值是 1.5 nM。
T28222	5-Hydroxy-1-methylhydantoin HD-003,HD003,5-羟基-1-甲基咪唑啉-2,4-二酮,NZ419,NZ-419,HD 003,NZ 419	Bradykinin Receptor	GPCR/G Protein
	5-Hydroxy-1-methylhydantoin (HD-003) 是一种可能用于治疗肾衰竭的抗氧化剂。它是肌酐代谢物，是一种羟基自由基清除剂，此前已显示通过抑制大鼠慢性肾病的进展来提供肾脏保护。它是一种新型抗氧化药物，可完全抑制 B2-激肽受体(B2KR) 对 VSMC 中高葡萄糖 (25 mM) 刺激的反应，并且还显示可减弱 BK 对 VSMC 重塑的影响。它抑制 BK 诱导的 MAPK 磷酸化增加并减弱 VSMC 中结缔组织生长因子 (CTGF) 蛋白水平的增加。这些研究结果表明，它可能通过其抗氧化特性赋予血管保护免受高葡萄糖浓度和 BK 刺激以改善血管损伤和重塑。
T19472	Nedocromil sodium Nedocromil disodium salt,FPL 59002KP	Others	Others
	Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling.
T28469	PT-262 PT 262
	PT-262 is a ROCK (Rho-associated coiled-coil forming protein kinase) inhibitor. It induces cytoskeleton remodeling and migration inhibition in lung carcinoma cells.
T28005	MDL-100240
	MDL-100240 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin with a balanced activity. MDL 100240 shows an impressive effectiveness both in preventing and in regressing hypertension-induced vascular remodeling and cardiac hypertrop
T36763	PAF C-18
	PAF C-18 is a naturally occurring phospholipid produced upon stimulation through two distinct pathways known as the remodeling" and 'de novo' pathways. It is less potent than PAF C-16 in the induction of platelet aggregation
T82308	GLP-2 (1-34) (human)
	GLP-2 (1-34) (human) 是一种肠道多肽，其在进食后数分钟内释放，并可用于研究骨重塑过程。
T61344	VO-OHPic
	VO-OHPic is a reversible, noncompetitive, and selective inhibitor of PTEN with an IC50 of 46 nM. It effectively attenuates apoptosis, adverse cardiac remodeling, and the presence of pro-inflammatory M1 macrophages in models of doxorubicin-induced cardiomyopathy. Additionally, VO-OHPic inhibits autophagy [1] [2] [3].
T39829	BPK-25
	BPK-25 is an active acrylamide compound that enhances the degradation of proteins in the nucleosome remodeling and deacetylation (NuRD) complex through a post-translational mechanism involving covalent protein interaction. Additionally, BPK-25 acts as an inhibitor of TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
T37268	PAF C-16 Carboxylic Acid
	PAF C-16 is a naturally occurring phospholipid produced upon stimulation through two distinct pathways known as the remodeling" and 'de novo' pathways. It is a potent mediator of neutrophil migration and the production of reactive oxygen species and IL-6. Pathological processes involving PAF include necrotizing enterocolitis
T39785	TH5427 hydrochloride
	TH5427 hydrochloride is a potent and selective inhibitor of NUDT5 with an IC50 of 29 nM. It demonstrates a remarkable 690-fold selectivity towards NUDT5 compared to MTH1. Moreover, TH5427 hydrochloride effectively inhibits progestin-dependent, PAR-derived nuclear ATP synthesis in breast cancer cells, thereby impeding chromatin remodeling, gene regulation, and ultimately suppressing proliferation.
T70748	Bisthianostat
	Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. Thi...
T70210	FT-1101 free base
	FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional r...
T36838	(R)-Bromoenol lactone
	The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β exce...
T80130	SDF-1α (human)	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SDF-1α (human) 是一种能够与CXCR4受体相结合的单核细胞趋化剂，它在心肌梗死模型中的干细胞归巢、维持、生存、增殖、心肌细胞修复、血管形成以及心室重构过程扮演关键角色。SDF-1α (human) 常用于心血管病研究。
T71110	Nanatinostat TFA
	Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor...
T35598	Neuromedin U-25 (human) (trifluoroacetate salt)
	Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery ...

化合物

Cat.No: T11394

Target: TRP/TRPV Channel

Cat.No: T23312

Target: 5-HT Receptor

Cat.No: T9765

Target: MyD88

Cat.No: T15418

Synonym: CVT-6883

Target: Adenosine Receptor

JQ-1 (carboxylic acid)

Cat.No: T5443

Synonym: JQ-1 carboxylic acid

Target: Epigenetic Reader Domain

Cat.No: T24115

Synonym: GSK-854,GSK 854

Target: Apoptosis

Cat.No: T9566

Target: Annexin A, YAP

Cat.No: T13360

Target: Autophagy

Cat.No: T77617

Target: MMP

Cat.No: T2129

Target: PDE

Rho-Kinase-IN-1

Cat.No: T12721

Target: ROCK

Cat.No: T21632

Target: Others, Microtubule Associated

Cat.No: T3661

Synonym: ACY241,HDAC-IN-2

Target: HDAC

Cat.No: T3712

Synonym: ABBV-075,米维布塞

Target: Apoptosis, Epigenetic Reader Domain

5-Hydroxy-1-methylhydantoin

Cat.No: T28222

Synonym: HD-003,HD003,5-羟基-1-甲基咪唑啉-2,4-二酮,NZ419,NZ-419,HD 003,NZ 419

Target: Bradykinin Receptor

Nedocromil sodium

Cat.No: T19472

Synonym: Nedocromil disodium salt,FPL 59002KP

Target: Others

Cat.No: T28469

Synonym: PT 262

Cat.No: T28005

Cat.No: T36763

GLP-2 (1-34) (human)

Cat.No: T82308

Cat.No: T61344

Cat.No: T39829

PAF C-16 Carboxylic Acid

Cat.No: T37268

TH5427 hydrochloride

Cat.No: T39785

Cat.No: T70748

FT-1101 free base

Cat.No: T70210

(R)-Bromoenol lactone

Cat.No: T36838

SDF-1α (human)

Cat.No: T80130

Target: CXCR

Nanatinostat TFA

Cat.No: T71110

Neuromedin U-25 (human) (trifluoroacetate salt)

Cat.No: T35598

Cat. No.	Product Name	Target	Signaling Pathways
T0543	7-Methylxanthine Heteroxanthine,Heteroxanthin,7-甲基黄嘌呤	Nucleoside Antimetabolite/Analog; Endogenous Metabolite	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	7-Methylxanthine (Heteroxanthine) 是一种黄嘌呤的甲基衍生物，是人尿结石的嘌呤成分。
T20089	ATP Atipi,ATP disodium salt hydrate,Triphosphoric acid adenosine ester,Ara-ATP,Triphosphaden,Adenosine triphosphate;Ara-ATP,Adenosine triphosphate	Endogenous Metabolite	Metabolism
	ATP (Adenosine triphosphate) 可为细胞提供能量，参与整体能量平衡，维持细胞内稳态。ATP 可以通过与特异性嘌呤能受体的相互作用充当细胞外信号分子，以介导神经传递、炎症、细胞凋亡和骨重塑等多种过程。
TN4819	(-)-Praeruptorin A	ATPase; IL Receptor; Calcium Channel; P-gp	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs.

天然产物

7-Methylxanthine

Cat.No: T0543

Synonym: Heteroxanthine,Heteroxanthin,7-甲基黄嘌呤

Target: Nucleoside Antimetabolite/Analog, Endogenous Metabolite

Cat.No: T20089

Synonym: Atipi,ATP disodium salt hydrate,Triphosphoric acid adenosine ester,Ara-ATP,Triphosphaden,Adenosine triphosphate;Ara-ATP,Adenosine triphosphate

Target: Endogenous Metabolite

(-)-Praeruptorin A

Cat.No: TN4819

Target: ATPase, IL Receptor, Calcium Channel, P-gp

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