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Search Results for " heterodimerization "

Targets Recommended: Others

11

抑制剂 & 化合物

1

天然产物

2

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T35862	Cucurbit[8]uril	Others	Others
	Cucurbit[8]uril is a highly effective and safe supramolecular compound that promotes protein heterodimerization. It selectively induces the heterodimerization of methylviologen and naphthalene functionalized proteins, demonstrating its specificity and versatility. Additionally, Cucurbit[8]uril shows exceptional oral activity and low toxicity, making it a promising candidate for various pharmaceutical and biotechnological applications.
T15396	GN44028 N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine	HIF	Angiogenesis; Chromatin/Epigenetic
	GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) 是缺氧诱导因子(HIF)-1的有效抑制剂，其 IC50=14 nM。它可以抑制低氧诱导的 HIF-1α 的转录特性，但不抑制 HIF-1α mRNA 的表达，HIF-1α 蛋白的累积或HIF-1α/HIF-1β 的异缘二聚化。
T0678	Amitriptyline hydrochloride Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin	Trk receptor; Sigma receptor; 5-HT Receptor; Serotonin Transporter; Sodium Channel; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
	Amitriptyline hydrochloride (Annoyltin) 是血清素再摄取转运体和去甲肾上腺素再摄取转运体抑制剂，还与多巴胺再摄取转运体结合，其Ki 为 2.58 μM。它也抑制肾上腺素能受体、毒蕈碱受体、组胺受体、5-羟色胺受体。它是TrkA 和TrkA 受体的激动剂，具有强神经营养活性和有抗抑郁作用。
T81646	NPAS3-IN-1	Others	Others
	NPAS3-IN-1 是一种有效的 NPAS3-ARNT 异二聚化抑制剂，通过在细胞层面上调控NPAS3与ARNT的异二聚化来调控 NPAS3的转录。
T12675L	PT2399	HIF/HIF Prolyl-Hydroxylase; HIF	Angiogenesis; Chromatin/Epigenetic; Metabolism
	PT2399 是高选择性的HIF-2α拮抗剂，能直接结合 HIF-2α PAS B 结构域，IC50=6 nM，具有显著的体内抗肿瘤特性。
T6760	APS-2-79 hydrochloride APS-2-79 HCl,APS-2-79	MEK; MAPK	MAPK
	APS-2-79 hydrochloride (APS-2-79 HCl) 是一种 KSR 依赖性的MEK 拮抗剂，可与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的KSR2。它与 KSR 结合可将 KSR 处于非活性状态，使其无法再结合 RAF 和激活 MEK，从而阻断 Ras-MAPK 信号通路。
T17009	TC-S 7009	HIF	Angiogenesis; Chromatin/Epigenetic
	TC-S 7009是一种有效的和具有选择性的HIF-2α抑制剂(Kd: 81 nM)。TC-S 7009对HIF-2α的亲和力大于HIF-1α (Kd >> 5 μM)。 TC-S 7009破坏HIF-2α异源二聚化，降低HIF-2α靶基因表达，降低dna 结合活性。
T69080	T1001	Others	Others
	T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.
T75943	TAT-cyclo-CLLFVY TFA
	TAT-cyclo-CLLFVY TFA 是一种 HIF-1异二聚化的环肽抑制剂，可抑制癌细胞中的缺氧信号传导。TAT-cyclo-CLLFVY TFA 破坏 HIF-1α/HIF-1β蛋白相互作用，IC50为 1.3 μM。
T79465	Anticancer agent 135	Androgen Receptor	Endocrinology/Hormones
	Anticanceragent 135（compound 26h）为一有效的雄激素受体（AR）拮抗剂，能够阻断AR核转位并抑制AR/AR-V7异二聚化，以抑制下游基因转录。该化合物在前列腺癌异种移植模型中展现出显著疗效。
T76893	Lusvertikimab
	Lusvertikimab (OSE-127) 是一种人源化IL7R 单克隆抗体。Lusvertikimab 不会被靶细胞内化并阻止 IL7R 异二聚化和随后的下游信号传导。Lusvertikimab 具有抗白血病功效，具有用于 B 细胞前体急性淋巴细胞白血病 (BCP-ALL) 研究的潜力。

化合物

Cucurbit[8]uril

Cat.No: T35862

Target: Others

Cat.No: T15396

Synonym: N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine

Target: HIF

Amitriptyline hydrochloride

Cat.No: T0678

Synonym: Amitriptyline HCl,Tryptizol,盐酸阿米替林,Domical,Annoyltin

Target: Trk receptor, Sigma receptor, 5-HT Receptor, Serotonin Transporter, Sodium Channel, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor

Cat.No: T81646

Target: Others

Cat.No: T12675L

Target: HIF/HIF Prolyl-Hydroxylase, HIF

APS-2-79 hydrochloride

Cat.No: T6760

Synonym: APS-2-79 HCl,APS-2-79

Target: MEK, MAPK

Cat.No: T17009

Target: HIF

Cat.No: T69080

Target: Others

TAT-cyclo-CLLFVY TFA

Cat.No: T75943

Anticancer agent 135

Cat.No: T79465

Target: Androgen Receptor

Cat.No: T76893

Cat. No.	Product Name	Target	Signaling Pathways
T5S2358	Dehydrocorydaline Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine	BCL; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Proteases/Proteasome
	Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节Bax，Bcl-2蛋白表达，激活caspase-7，caspase-8，并使PARP 失活。它能增强p38 MAPK 活化，具有抗炎、抗癌等功效。它具有强大的抗疟疾作用，并具低细胞毒性。

天然产物

Dehydrocorydaline

Cat.No: T5S2358

Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine

Target: BCL, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-01203	RP2 Protein, Human, Recombinant (GST) DELXp11.3,RP2,NME10,KIAA0215,NM23-H10,TBCCD2,retinitis pigme...	Human	Baculovirus Insect Cells
	XRP2, also known as Protein XRP2 and RP2, is a member of the TBCC (tubulin cofactor C) family and contains one C-CAP/cofactor C-like domain. This protein is encoded by the RP2 gene in humans. XRP2 stimulates the GTPase activity of tubulin, but does not enhance tubulin heterodimerization. XRP2 acts as guanine nucleotide dissociation inhibitor for ARL3. Defects in RP2 gene are the cause of retinitis pigmentosa type 2 (RP2), also known as X-linked retinitis pigmentosa 2 (XLRP-2). It leads to degene...
TMPH-01280	EGLN1 Protein, Human, Recombinant (His & Myc) HPH-2,EGLN1,PHD2,SM-20,HIF-prolyl hydroxylase 2,HIF-PH2,C1or...	Human	E. coli
	Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific proline found in each of the oxygen-dependent degradation (ODD) domains (N-terminal, NODD, and C-terminal, CODD) of HIF1A. Also hydroxylates HIF2A. Has a preference for the CODD site for both HIF1A and HIF1B. Hydroxylated HIFs are then targeted for proteasomal degradation via the von Hippel-Lindau ubiquiti...

重组蛋白

RP2 Protein, Human, Recombinant (GST)

Cat.No: TMPY-01203

Species: Human

Expression System: Baculovirus Insect Cells

EGLN1 Protein, Human, Recombinant (His & Myc)

Cat.No: TMPH-01280

Species: Human

Expression System: E. coli

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