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Search Results for " conformation "

53

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP1263	Fz7-21 (Ac)-LPSDDLEFWCHVMY-NH2	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Fz7-21 ((Ac)-LPSDDLEFWCHVMY-NH2) 是一种 Frizzled 7 (FZD 7) 受体的肽抑制剂，能够选择性的与FZD7 CRD 亚类结合。它还阻断了WNT3A 介导的β-catenin 在小鼠L 细胞中的稳定作用。它对外源性WNT3A 刺激和转染WNT3A 或WNT1的HEK293细胞Wnt/β-catenin 信号传导有损伤。
T28267L	(+)-ORM-10921	Others	Others
	(+)-ORM-10921 是 ORM-10921 的一种构型，可用于化学合成方面的研究。
T34760	SYR127063 SYR-127063,BDBM 92454,SYR 127063,BDBM-92454,BDBM92454	EGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	SYR127063 (BDBM-92454) 是一种有效的选择性 HER2 抑制剂，以反应构象与 HER2 结合。
T19802	B-Raf IN 11	Raf	MAPK
	B-Raf IN 11 是一种新型选择性抑制剂。 B-Raf 激酶V600E 突变体的DFG-in 构象优于结肠直肠癌中的DFG-out 构象。
T25210	CBHcy	Transferase	Metabolism
	CBHcy 是一种双底物类似物，是一种特异性 BHMT 抑制剂，可使甜菜碱-同型半胱氨酸 S-甲基转移酶（BHMT）采用与三元配合物相同的构象，可能会诱导半胱氨酸血症的发生。
T5938	4-Phenoxybenzylamine	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	4-Phenoxybenzylamine 通过稳定无活性构象来抑制NS3蛋白的功能，对 HCV NS3/4a 的 IC50 约为 500 μM。
T21648	CP-31398 dihydrochloride CP 31398 dihydrochloride	p53	Apoptosis
	CP-31398 dihydrochloride 是一种 p53 稳定剂，可稳定 p53 的活性构象并促进具有突变型或野生型 p53 的癌细胞系中的 p53 活性。
T37807	JTV 519 fumarate
	Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo. Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]ryanodine binding to RyR2 irrespective of FKBP12.6 association. Biochem.J. 404 431 PMID:17313373 \|Chen et al (2008) Effect of K201, a novel antiarrhythmic drug on calcium handling and arrhythmogenic activity of pulmonary vein cardiomyocytes. Br.J.Pharmacol. 153 915 PMID:17994112 \|...
T8864	Thymidylate Kinase Inhibitor, YMU1	Others	Others
	YMU1 是一种选择性抑制剂，特异性作用于人胸苷酸激酶 (IC50: 610 nM) 。
T22980	MIRA-1 p53 Activator VIII,1-[(1-Oxopropoxy)methyl]-1H-pyrrole-2,5-dione,(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate,NSC 19630,WRN Helicase Inhibitor	DNA/RNA Synthesis; p53	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	MIRA-1 (WRN Helicase Inhibitor) 是马来酰亚胺类似物。它可以恢复p53依赖的转录转激活诱导 p53 突变细胞凋亡，具有抗肿瘤作用。
T8655	SR-717	STING	Immunology/Inflammation
	SR-717 是一种 cGAMP 的类似物，一种非核苷类 STING 激动剂，可以诱导 STING 形成“封闭”的激活构象。SR-717 具有抗肿瘤活性，可以促进免疫细胞的激活以及抗原的交叉提呈。
T9095	Necrostatin-34 2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4	RIP kinase	Apoptosis; NF-κB
	Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) 是一种 RIPK1 激酶抑制剂，通过在激酶结构域中占据一个独特的结合口袋，将 RIPK1 激酶稳定在非活性构象中。
T4414	Eprenetapopt APR-246,PRIMA-1Met	Apoptosis; Others; Ferroptosis; p53; Autophagy	Apoptosis; Autophagy; Others
	Eprenetapopt (PRIMA-1Met) 是一种在 TP53突变细胞中恢复野生型 p53功能的小分子，可引发肿瘤细胞凋亡，还抑制硒蛋白硫氧还蛋白还原酶 1。
T8684	Sotorasib AMG-510	Ras	GPCR/G Protein; MAPK
	Sotorasib (AMG-510) 是一种 KRAS G12C 共价抑制剂，具有口服活性和选择性。Sotorasib 与 KRAS G12C 非活性构象的 GDP 状态结合，抑制 KRAS 及其下游信号的传导。Sotorasib 对 KRAS G12C 突变肿瘤具有抑制活性。
T24076	FzM1 FzM 1,FzM-1	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	FzM1 是卷曲蛋白受体 FZD4 的负变构调节剂 (NAM)。 FzM1减少 WNT5A 依赖的 WNT 反应元件 (WRE) 活性 (log EC50inh=-6.2)。 FzM1 与位于 FZD4 细胞内环 3 (ICL3) 的变构结合位点结合并改变受体的构象，从而抑制 WNT/β-连环蛋白级联反应。
T8799	(E/Z)-IT-603 IT603	Others; NF-κB	NF-κB; Others
	(E/Z)-IT-603 是一种c-Rel 抑制剂，其IC50=3 μM。它是 E-IT-603 和 Z-IT-603的混合物。它具有抗癌作用。它有望作为调节剂调节移植物抗宿主病和恶性病中的 T 细胞反应。
T8369	Adagrasib MRTX849	Ras	GPCR/G Protein; MAPK
	Adagrasib (MRTX849) 是一种 KRAS G12C 共价抑制剂，具有口服活性和选择性。Adagrasib 与 KRAS G12C 非活性构象的 GDP 状态结合，抑制 KRAS 及其下游信号的传导。Adagrasib 对 KRAS G12C 突变肿瘤具有抑制活性。
T61822	M1002	HIF	Angiogenesis; Chromatin/Epigenetic
	M1002 是一种缺氧诱导因子-2 (HIF-2) 激动剂，可以增强HIF-2alpha和ARNT对转录激活的亲和力。M1002能够改变HIF-281alpha PAS-B结构域的Tyr2构象，与脯氨酰羟化酶结构域 (PHD) 抑制剂可发挥协同作用。
T10826	CK-666	HIV Protease; Microtubule Associated	Cytoskeletal Signaling; Microbiology/Virology; Proteases/Proteasome
	CK-666 是一种肌动蛋白相关蛋白 Arp2/3 复合物的细胞渗透性抑制剂。它与 Arp2/3 复合物结合，稳定复合物的非活性状态，阻止 Arp2 和 Arp3 亚基进入活化的丝状短节距构象。
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)	Trk receptor	Tyrosine Kinase/Adaptors
	Cyclotraxin B acetate(1203586-72-4 free base) 是 TrkB 受体的拮抗剂；抑制 BDNF 诱导的 TrkB 活性 (IC50 = 0.30 nM)。变构改变 TrkB 受体构象但不改变 BDNF 结合。防止 BDNF 引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。
T9172	Simufilam dihydrochloride PTI-125 dihydrochloride	Others	Others
	Simufilam dihydrochloride (PTI-125 dihydrochloride) 是口服具有活力的、毒性低的 filamin A 激活剂。它可优先结合改变的 FLNA，并恢复其天然构象，恢复受体和突触活性，并减少其与 a7nAChR/TLR4 的关联和下游病理作用。它可用于研究阿尔茨海默症。
T16538	PIN1 inhibitor API-1	Others	Others
	PIN1 inhibitor API-1 是特殊的 Pin1抑制剂，可直接特异性地与 Pin1 肽基脯氨酰异构酶结构域结合，并抑制 Pin1 顺反异构活性。它保留 pXPO5 的活性构象，恢复 pXPO5 将前 miRNA 从细胞核转运到细胞质的能力，从而上调抗癌 miRNA 的生物发生，抑制体内外肝癌的发生。
T69246	J-31
	J-31 is an inactive conformation inhibitor of ITK.
T40536	[Glu4]-Oxytocin [Glu4]-Oxytocin
	[Glu4]-Oxytocin is a suitable derivative of oxytocin for conducting a thorough investigation, utilizing various methods, into the conformation of "oxytocin-like" molecules in aqueous solution.
T38599	HPK1-IN-8 HPK1-IN-8
	HPK1-IN-8 is an allosteric inhibitor that selectively targets the inactive conformation of full-length HPK1.
T26450	A 80915A A80915A,A-80915A
	A 80915A is A semi-naphthoquinone antibiotic from Streptomyces aculeolatus. It is a potent inhibitor of gastric (H(+)-K+)-ATPase. Inhibition by A80915A is dependent on the conformation of gastric (H(+)-K+)-ATPase, potassium slows the rate of inhibition by
T38439	DC-Srci-6649
	DC-Srci-6649 is a potent and selective inhibitor of c-Src kinase, effectively blocking its phosphorylation and stabilizing it in an inactive conformation.
TP1311	RGD peptide (GRGDNP) (TFA) (114681-65-1 free base) RGD peptide (GRGDNP) (TFA)
	RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
T35887	MBD
	MBD, a novel fluorescent probe (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), is utilized to study the conformation of protein and nucleoprotein. Its application is extended to bacterial ribosomes, as well as bovine trypsinogen and trypsin. MBD exhibits significant fluorescence when it binds to the hydrophobic region of macromolecules [1][2].
T71747	IKKß-IN-124
	IKKß-IN-124 is an allosteric inhibitor of IκBα phosphorylation and NF-κB transcriptional activity through selective capture of the inactive conformation and hence blockade of IKKβ S177/S181 phosphorylation.
T39313	KALA
	KALA, an amphiphilic peptide, adopts an α-helical conformation under physiological pH conditions. It functions as a fusogenic peptide, modifying the liposomal membrane that encapsulates plasmid DNA, thereby facilitating liver targeting and DNA transfection through galactose receptors.
T29086	VA5 TG2 inhibitor VA5,VA-5,VA 5
	VA5 is an transamidase inhibitor by direct binding at the transamidase site. VA5 also inhibits GTP-binding activities. It interaction at the transamidase site locks the protein in the extended/open conformation to disorganize/inactivate the GTP binding/GT
TP2068	Cyclotraxin B
	Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p
T80057	Cytochrome P450 reductase
	Cytochrome P450reductase，一种NADPH-细胞色素还原酶，发挥作用于促进芳香酶构象，以最适合底物结合。
T12068	MK-8033 hydrochloride	Others	Others
	MK-8033 hydrochloride 是一种有效的、具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂，对c-Met 的为1 nM ，对Ron 的IC50为7nM。MK-8033 hydrochloride 对活化的激酶构象 (activated kinase conformation)具有很高的亲和力，可用于乳腺癌，膀胱癌、非小细胞肺癌 (NSCLC)等癌症的研究。
T61664	Benzoquinoquinoxaline
	Benzoquinoquinoxaline (BQQ) is a heterocyclic compound featuring an aminoalkyl side chain. BQQ exhibits preferential binding to DNA triplex structures, intercalating between the bases to stabilize the triplex conformation. Additionally, conjugation of BQQ to 1,10-phenanthroline enables specific binding and cleavage of double-strand DNA at the site where a triplex structure forms [1].
T36803	AAQ chloride
	Photoswitchable Kv channel blocker (IC50 values are 2 and 64 μM at 500 nm and 380 nm respectively). Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Exhibits minimal activity at Nav1.2 and L-type Ca2+ channels. Stimulates action potential firing of hippocampal neurons in vitro at 500 nm and restores visual responsiveness in blind mice at 380 nm. Fortin et al (2008) Photochemical control of endogenous ion channels and cellular excitability. Nat.Methods 5 331 PMID:1831...
T78378	PK7088	Others	Others
	PK7088是一种结合了吡唑结构与特定肽序列的化合物，能够促使突变型p53恢复为具有野生型特性的形式，从而实现突变型p53的重激活。在癌症研究中，PK7088显示出其抗肿瘤活性。
T62885	GABAA receptor modulator-2
	GABAA receptor modulator-2 (Compound 20) 是一种选择性的、口服具有活力的 α5-GABAAR 负向变构调节剂 (Ki: 4.1 nM)。GABAA receptor modulator-2 表现出高代谢稳定性、良好的中枢神经系统安全性。
T68473	WAY-255348
	WAY-255348 is a potent nonsteroidal progesterone receptor (PR) antagonist. WAY-255348 inhibits the activity of progesterone. WAY-255348 achieves antagonist activity by binding to and subsequently preventing progesterone-induced nuclear accumulation, phosphorylation and promoter interactions of the PR. WAY-255348 bound PR conformation was similar to that of a progesterone agonist-bound PR and distinct from steroidal antagonist-bound PR conformations. WAY-255348 inhibits PR action through a novel ...
T9569	simufilamum
	Simufilam 是一种低毒，口服的 filamin A (FLNA) 激活剂。Simufilam 优先结合大脑中改变的FLNA，恢复其天然构象，恢复受体和突触活性，并减少其与 a7nAChR/TLR4 的关联和下游病理作用。Simufilam 可用于阿尔茨海默症的研究。
T63549	MRGPRX1 agonist 4
	MRGPRX1 agonist 4 是有效的、口服具有活力的 Mas 相关 G 蛋白偶联受体 X1 (MRGPRX1)正向变构调节剂 (EC50: 0.1 μM)。MRGPRX1 agonist 4 表现出良好的代谢稳定性以及口服生物利用度。MRGPRX1 agonist 4 能够改善人源性 MRGPRX1 神经疼痛模型小鼠行为性热过敏反应。
TP2182	Lamin fragment	Others	Others
	Lamin fragment has a peptide sequence of Lys-Ala-Gly-Gln-Val-Val-Thr-Ile-Trp. Lamin polypeptides have an almost complete α-helical conformation with multiple α-helical domains separated by non-α-helical linkers that are highly conserved in length and amin
T36956	Bis-ANS dipotassium 4,4'-Dianilino-1,1'-binaphthyl-5,5'-disulfonic Acid,bis-ANS (potassium salt)
	bis-ANS is a high-affinity non-covalent extrinsic fluorescent dye used to analyze protein conformation.[1] Its predominant interaction with proteins is through its hydrophobic phenyl and naphthyl rings.[2] bis-ANS has an excitation maxima of 390 nm.[3] It has an emission maximum of 523 nm when free in solution but undergoes a blue shift with an increase in fluorescence intensity when bound to protein; for example, when bound to intestinal fatty acid binding protein (FAPB2) it has emission maxima...
T38219	11-cis Retinal
	11-cis Retinal is a chromophore that binds to opsin in the mammalian visual system as an inverse agonist forming the inactive conformation of rhodopsin. When 11-cis retinal absorbs a photon of light, it isomerizes to form all-trans retinal beginning the phototransduction cycle, which is the basis for mammalian vision. A G121L mutation in opsin allows 11-cis retinal to bind as a partial agonist and activate rhodopsin in the absence of light. In a moth model of carotenoid deficiency-induced low vi...
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。
T36017	PF-05381941
	PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively[1]. PF-05381941 inhibits LPS-stimulated release of TNF-αfrom human peripheralmononuclear (PMN) cells with an IC50 of 8 nM[1]. [1]. Kilty I, et al. TAK1 inhibition in the DFG-out conformation. Chem Biol Drug Des. 2013;82(5):500-505.
T79013	SLMP53-2
	SLMP53-2是一种可以重建p53转录活性的突变p53再激活因子。该化合物通过促进mutp53-Y220C与Hsp70之间的作用，恢复了mutp53-Y220C的野生型构象和其DNA结合能力。此外，SLMP53-2能够诱导细胞周期停滞、细胞凋亡以及ER应激，展现出了其抗肿瘤的潜力。
T60635	Simufilam hydrochloride
	Simufilam (PTI-125) (hydrochloride) 是一种具有口服活性的细丝蛋白 A (FLNA) 激活剂，具有低毒性，可用于阿尔茨海默病研究。Simufilam (hydrochloride) 优先结合改变的细丝蛋白 A 并恢复其天然构象，恢复受体和突触活性，并减少其与 a7nAChR/TLR4 的关联和下游病理作用。
T35928	NVS-PAK1-C NVS-PAK1-C
	NVS-PAK1-C 是一种有效的、ATP 竞争的特异性变构 PAK1抑制剂探针。NVS-PAK1-C 可抑制去磷酸化的 PAK1(IC50= 5 nM) 和磷酸化的 PAK1(IC50= 6 nM)。NVS-PAK1-C 也可以抑制去磷酸化的 PAK2 (IC50=270 nM) 和磷酸化的 PAK2 (IC50=720 nM)。

化合物

Cat.No: TP1263

Synonym: (Ac)-LPSDDLEFWCHVMY-NH2

Target: Wnt/beta-catenin

Cat.No: T28267L

Target: Others

Cat.No: T34760

Synonym: SYR-127063,BDBM 92454,SYR 127063,BDBM-92454,BDBM92454

Target: EGFR, HER

Cat.No: T19802

Target: Raf

Cat.No: T25210

Target: Transferase

4-Phenoxybenzylamine

Cat.No: T5938

Target: HCV Protease

CP-31398 dihydrochloride

Cat.No: T21648

Synonym: CP 31398 dihydrochloride

Target: p53

JTV 519 fumarate

Cat.No: T37807

Thymidylate Kinase Inhibitor, YMU1

Cat.No: T8864

Target: Others

Cat.No: T22980

Synonym: p53 Activator VIII,1-[(1-Oxopropoxy)methyl]-1H-pyrrole-2,5-dione,(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate,NSC 19630,WRN Helicase Inhibitor

Target: DNA/RNA Synthesis, p53

Cat.No: T8655

Target: STING

Cat.No: T9095

Synonym: 2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4

Target: RIP kinase

Cat.No: T4414

Synonym: APR-246,PRIMA-1Met

Target: Apoptosis, Others, Ferroptosis, p53, Autophagy

Cat.No: T8684

Synonym: AMG-510

Target: Ras

Cat.No: T24076

Synonym: FzM 1,FzM-1

Target: Wnt/beta-catenin

Cat.No: T8799

Synonym: IT603

Target: Others, NF-κB

Cat.No: T8369

Synonym: MRTX849

Target: Ras

Cat.No: T61822

Target: HIF

Cat.No: T10826

Target: HIV Protease, Microtubule Associated

Cyclotraxin B acetate(1203586-72-4 free base)

Cat.No: TP2068L

Target: Trk receptor

Simufilam dihydrochloride

Cat.No: T9172

Synonym: PTI-125 dihydrochloride

Target: Others

PIN1 inhibitor API-1

Cat.No: T16538

Target: Others

Cat.No: T69246

[Glu4]-Oxytocin

Cat.No: T40536

Synonym: [Glu4]-Oxytocin

Cat.No: T38599

Synonym: HPK1-IN-8

Cat.No: T26450

Synonym: A80915A,A-80915A

Cat.No: T38439

RGD peptide (GRGDNP) (TFA) (114681-65-1 free base)

Cat.No: TP1311

Synonym: RGD peptide (GRGDNP) (TFA)

Cat.No: T35887

Cat.No: T71747

Cat.No: T39313

VA5 TG2 inhibitor

Cat.No: T29086

Synonym: VA5,VA-5,VA 5

Cat.No: TP2068

Cytochrome P450 reductase

Cat.No: T80057

MK-8033 hydrochloride

Cat.No: T12068

Target: Others

Benzoquinoquinoxaline

Cat.No: T61664

Cat.No: T36803

Cat.No: T78378

Target: Others

GABAA receptor modulator-2

Cat.No: T62885

Cat.No: T68473

Cat.No: T9569

MRGPRX1 agonist 4

Cat.No: T63549

Cat.No: TP2182

Target: Others

Bis-ANS dipotassium

Cat.No: T36956

Synonym: 4,4'-Dianilino-1,1'-binaphthyl-5,5'-disulfonic Acid,bis-ANS (potassium salt)

Cat.No: T38219

Cat.No: T80859

Cat.No: T36017

Cat.No: T79013

Simufilam hydrochloride

Cat.No: T60635

Cat.No: T35928

Synonym: NVS-PAK1-C

Cat. No.	Product Name	Target	Signaling Pathways
T5S2361	Epiberberine	ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE	Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling
	Epiberberine 是一种从黄连中得到的生物碱，是AChE 和BChE 抑制剂，和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期，它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用，能够清除 ONOO-，可用于阿尔滋海默症和糖尿病的研究。

天然产物

Cat.No: T5S2361

Target: ERK, Beta-Secretase, MEK, BACE, AMPK, AChR, AChE

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