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29

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T60303	Collagen-IN-1
	Collagen-IN-1 (compound 3) is an ortho-carbonyl hydroquinone derivative exhibiting selective inhibition of collagen. It non-competitively inhibits agonist-induced platelet aggregation, with an IC50 value of 1.77 μM. Collagen-IN-1 effectively reduces the expression of P-selectin, activation of glycoprotein IIb/IIIa, and release of adenosine triphosphate and CD63 from platelets. This compound holds promise for research into platelet-related thrombosis diseases [1].
T2386	Pirfenidone S-7701,AMR-69,S-7701,AMR69,吡非尼酮	CCR; TGF-beta/Smad	Immunology/Inflammation; Microbiology/Virology; Stem Cells
	Pirfenidone (AMR69) 是一种抗纤维化剂，可减弱纤维细胞中CCL2和CCL12的产生。它可抑制细胞生长，并能降低人胶质瘤细胞系中的TGF-β2蛋白水平，具有抗炎活性。
T24816	SP-100030 SP100030,SP 100030	NF-κB	NF-κB
	SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat 和其他T 细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。
T38294	4-Deoxypyridoxine hydrochloride	S1P Receptor	GPCR/G Protein
	4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T80025	Bovine Type II Collagen Collagen, Type II, Immunization Grade
	Type II collagen 是一种治疗骨关节炎的有效蛋白质。在减缓小鼠胶原性关节炎疼痛和炎症方面，Type II collagen 显示了显著的效果。
T35725	4-hydroxy Valsartan
	4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.
T78030	GRGESP
	GRGESP为胶原凝胶收缩抑制剂，能够抑制人成纤维细胞在胶原凝胶中的扩散，显著减少凝胶收缩，适用于结缔组织形态发生研究。
T36930	Palmitoyl Tetrapeptide-7 (acetate)
	Palmitoyl tetrapeptide-7 is a cosmeceutical peptide that stimulates type I collagen, fibronectin, and hyaluronic acid production in skin.1Formulations containing palmitoyl tetrapeptide-7 have been used in the treatment of photoaging, dark circles, and undereye puffiness. 1.Bucay, V.W., and Day, D.Adjunctive skin care of the brow and periorbital regionClin. Plast. Surg.40(1)225-236(2013)
T36929	Pal-KTTKS (acetate)
	Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS...
T60557	TRAP-6-IN-1
	TRAP-6-IN-1 (Compound 8) 是胶原蛋白和TRAP-6的双重抑制剂，IC50值分别为 17.12 μM 和 11.88 μM。TRAP-6-IN-1 非竞争性抑制激动剂诱导的血小板聚集。
TP2186	PalMitoyl Tripeptide-1	Others	Others
	PalMitoyl Tripeptide-1 对人体皮肤成纤维细胞中胶原蛋白、纤连蛋白和透明质酸的合成有影响，可用于制备抗衰老化妆品。
TP2186L1	PalMitoyl Tripeptide-1 hydrochloride PalMitoyl Tripeptide-1 hydrochloride(147732-56-7 Free base),棕榈酰三肽-1盐酸盐	Others	Others
	PalMitoyl Tripeptide-1 hydrochloride (PalMitoyl Tripeptide-1 hydrochloride (147732-56-7 Free base)) 对人体皮肤成纤维细胞中胶原蛋白、纤连蛋白和透明质酸的合成有影响，可用于制备抗衰老化妆品。
T82780	Caprooyl-tetrapeptide-3 acetate
	Caprooyl-tetrapeptide-3 acetate 旨在减少细纹与皱纹。该化合物能够在皮质激素诱导的皮肤老化模型中刺激VII型胶原蛋白及层粘连蛋白5的表达。
T80859	Vitronectin
	Vitronectin为一类多功能糖蛋白，广泛分布于血液及细胞外基质。该蛋白质与糖胺聚糖、胶原蛋白、纤溶酶原及尿激酶受体发生结合，并对纤溶酶原激活抑制剂1的抑制构象起稳定作用。Vitronectin常用于促进伤口愈合和肿瘤进展研究领域。
T61586	TGFβ-IN-2
	TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].
T73770	Galactosylhydroxylysine hydrochloride
	Galactosylhydroxylysine hydrochloride, 一种羟基赖氨酸经糖基化转换后生成的骨胶原蛋白成分，该化合物在骨吸收过程中释放，其浓度在代谢性骨丢失疾病中会上升。
T41079	MMP13-IN-2 MMP13-IN-2
	MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.
T78219	Obtustatin triacetate	Integrin	Cytoskeletal Signaling
	Obtustatin triacetate 是一种从 Vipera lebetina obtusa 毒液中提取、含有 41 个残基的非 RGD 型解整合素。它作为整合素α1β1与 IV 型胶原蛋白粘附的高效且选择性抑制剂，能够抑制血管生成，因此在癌症研究中有应用。
T36101	Psychotridine
	Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol...
T79260	MCI	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	MCI具有针对性地清除活性氧(ROS)并降低环氧合酶-2(COX-2)表达的功能，COX-2的IC50值为1.23μM。在胶原诱导的关节炎(CIA)模型中展现出的抗炎效果明显，适用于类风湿性关节炎(RA)的研究。
T74632	TP0556351	MMP	Proteases/Proteasome
	TP0556351是一种高效且选择性地抑制基质金属蛋白酶2 (MMP2) 的化合物，其IC50值为0.2 nM。在Bleomycin诱导的肺纤维化小鼠模型中，该化合物能显著减少肺部胶原蛋白的含量，适用于特发性肺纤维化(IPF)的研究。
T69671	SR1903 TFA
	SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-190...
T81592	Osteostatin PTHrP (107–111)
	Osteostatin为甲状旁腺激素相关蛋白(PTHrP) 107-111片段，该化合物在动物模型中促进骨缺损修复，预防炎症性关节炎引起的骨侵蚀，并抑制骨胶原诱导的关节炎及破骨细胞的吸收作用。Osteostatin主要应用于免疫炎症的研究领域。
T60854	ENMD-1068 hydrochloride
	ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。
T35638	SR 1903
	SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of th...
T35695	Oleic Acid-13C
	Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximate...
T74142	Angiotensin II human TFA
	Angiotensin II human (Angiotensin II) TFA 作为肾素/血管紧张素系统中关键的生物活性肽，扮演着血管收缩剂的角色并在调节人体血压中发挥中心作用。其主要通过与 G 蛋白偶联受体 (GPCRs)、血管紧张素 II 1型受体 (AT1R) 和血管紧张素 II 2型受体 (AT2R) 的相互作用来介导效应，包括刺激交感神经系统、增加醛固酮的生物合成和肾脏功能。此外，Angiotensin II human TFA 促进血管平滑肌细胞的生长和 I 型及 III 型胶原在成纤维细胞中的合成，导致血管壁与心肌增厚及纤维化，并诱导细胞凋亡。还通过LOX-1依赖的氧化还原敏感路径诱导内皮细胞中的毛细血管形成。
T36486	Benpyrine
	Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abo...
T36717	RWJ-56110 dihydrochloride
	RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap...

化合物

Collagen-IN-1

Cat.No: T60303

Cat.No: T2386

Synonym: S-7701,AMR-69,S-7701,AMR69,吡非尼酮

Target: CCR, TGF-beta/Smad

Cat.No: T24816

Synonym: SP100030,SP 100030

Target: NF-κB

4-Deoxypyridoxine hydrochloride

Cat.No: T38294

Target: S1P Receptor

Bovine Type II Collagen

Cat.No: T80025

Synonym: Collagen, Type II, Immunization Grade

4-hydroxy Valsartan

Cat.No: T35725

Cat.No: T78030

Palmitoyl Tetrapeptide-7 (acetate)

Cat.No: T36930

Pal-KTTKS (acetate)

Cat.No: T36929

Cat.No: T60557

PalMitoyl Tripeptide-1

Cat.No: TP2186

Target: Others

PalMitoyl Tripeptide-1 hydrochloride

Cat.No: TP2186L1

Synonym: PalMitoyl Tripeptide-1 hydrochloride(147732-56-7 Free base),棕榈酰三肽-1盐酸盐

Target: Others

Caprooyl-tetrapeptide-3 acetate

Cat.No: T82780

Cat.No: T80859

Cat.No: T61586

Galactosylhydroxylysine hydrochloride

Cat.No: T73770

Cat.No: T41079

Synonym: MMP13-IN-2

Obtustatin triacetate

Cat.No: T78219

Target: Integrin

Cat.No: T36101

Cat.No: T79260

Target: Reactive Oxygen Species

Cat.No: T74632

Target: MMP

Cat.No: T69671

Cat.No: T81592

Synonym: PTHrP (107–111)

ENMD-1068 hydrochloride

Cat.No: T60854

Cat.No: T35638

Cat.No: T35695

Angiotensin II human TFA

Cat.No: T74142

Cat.No: T36486

RWJ-56110 dihydrochloride

Cat.No: T36717

Cat. No.	Product Name	Target	Signaling Pathways
TN6975	Cirsiumaldehyde 5,5’-oxydimethylenebis(2-furfural)	Platelet aggregation	Others
	Cirsiumaldehyde 是一种从Lobelia chinensis、Cornus officinalis 成熟果实和 Hippophae rhamnoides 果实中分分离出的化合物。Cirsiumaldehyde 在胶原蛋白存在下对 U46619 诱导（1~5 uM）的大鼠血小板聚集的抑制浓度为 0.8~1.0 ug/mL。
T2769	3-Aminopropionitrile fumarate (2:1) Di-β-aminopropionitrile fumarate,3-Aminopropionitrile fumarate,3-氨基丙腈,β-Aminopropionitrile fumarate,3-Aminopropionitrile fumarate 2:1,Beta-Aminopropionitrile fumarate,β-Ammoniumpropionitrile hemifumarate	Others	Others
	3-Aminopropionitrile fumarate (2:1) (β-Aminopropionitrile fumarate) 是一种能抑制胶原蛋白(collagen)交联的山黧豆素。
T4S0498	Glaucocalyxin A 蓝萼甲素,Wangzaozin B,Leukamenin F	Apoptosis; Akt; Caspase; PI3K	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。
T79983	Flaccidoside II	Apoptosis	Apoptosis
	Flaccidoside II 是一种源自Anemone flaccida根茎的三萜皂苷，能抑制恶性周围神经鞘瘤(MPNST)细胞系增殖并诱导细胞凋亡(apoptosis)。此外，Flaccidoside II 亦能改善由胶原蛋白引发的小鼠关节炎症状。
T38330	Collinin
	Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a...
T35624	Ajoene
	Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...

天然产物

Cirsiumaldehyde

Cat.No: TN6975

Synonym: 5,5’-oxydimethylenebis(2-furfural)

Target: Platelet aggregation

3-Aminopropionitrile fumarate (2:1)

Cat.No: T2769

Synonym: Di-β-aminopropionitrile fumarate,3-Aminopropionitrile fumarate,3-氨基丙腈,β-Aminopropionitrile fumarate,3-Aminopropionitrile fumarate 2:1,Beta-Aminopropionitrile fumarate,β-Ammoniumpropionitrile hemifumarate

Target: Others

Glaucocalyxin A

Cat.No: T4S0498

Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F

Target: Apoptosis, Akt, Caspase, PI3K

Flaccidoside II

Cat.No: T79983

Target: Apoptosis

Cat.No: T38330

Cat.No: T35624

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