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41

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8469 LQZ-7I

Survivin Apoptosis
LQZ-7I 能口服有效地抑制异种移植肿瘤生长并诱导肿瘤中生存素的损失。它是一种靶向生存素的抑制剂,抑制生存素二聚化。
T5697 BMS-1166

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
BMS-1166 是 PD-1/PD-L1免疫检查点抑制剂。它促使 PD-L1 形成 PD-L1 同源二聚体,进而阻断其与 PD-1 的相互作用,其 IC50为 1.4 nM。它阻断了 PD-1/PD-L1 免疫检查点对 T 细胞活化的抑制作用。
T4367 Mycro 3

Mycro-3

c-Myc; Autophagy Autophagy; Cell Cycle/Checkpoint
Mycro 3 在全细胞分析中对 c-Myc 具有强效选择性,可用于胰腺癌的研究。
T3686 10074-G5

c-Myc; Autophagy Autophagy; Cell Cycle/Checkpoint
10074-G5是一种c-Myc-Max 二聚化的抑制剂,IC50值为146 μM。
T21083 TFIIH Modulator-19

TFIIH Modulator19,TFIIH Modulator 19

Others Others
TFIIH Modulator-19 诱导毛发硫营养不良组 A 蛋白的二聚化以调节 TFIIH 转录活性。
T35074 VRT-325

CFcor 325,VRT-534,CFcor325,VRT 325,VRT325,CF-106951,CFcor-325

Others Others
VRT-325 可以通过促进两个 NBD 的二聚化或促进 TMD 的折叠来修复折叠缺陷。VRT-325 可加速CF细胞单层的愈合速度。
T21082 2,5-Dihydroxybiphenyl

TFIIH Modulator 12,2,5-二羟基联苯,TFIIH Modulator12

Others Others
2,5-Dihydroxybiphenyl (TFIIH Modulator12) 是一种小分子去稳定诱导剂,可诱导毛发硫营养不良组 A 蛋白的二聚化,从而调节 TFIIH 转录活性。
T6818 DEL-22379

DEL22379

Apoptosis; ERK Apoptosis; MAPK
DEL-22379 是一种水溶性 ERK 二聚化抑制剂,IC50约为 0.5 μM。
T7184 Firsocostat

ND-630,NDI-010976,GS-0976

Acetyl-CoA Carboxylase Metabolism
Firsocostat (GS-0976) 是有效的乙酰辅酶A 羧化酶 (ACC) 抑制剂,抑制人类 ACC1 和 ACC2 的IC50分别为2.1和6.1 nM。
T60160 STX-0119

STAT JAK/STAT signaling; Stem Cells
STX-0119 是一种选择性的、具有口服活性的 STAT3 二聚抑制剂。STX-0119 抑制 STAT3 转录,IC50 为 74 μM。
T6908 NSC 228155

NSC228155

EGFR; Epigenetic Reader Domain; DNA/RNA Synthesis; Histone Acetyltransferase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; JAK/STAT signaling; Tyrosine Kinase/Adaptors
NSC 228155 是一种 EGFR 的激活剂,与 sEGFR 二聚化结构域 II 结合并调节 EGFR 酪氨酸磷酸化。
T9909 Pertuzumab

帕妥珠单抗,帕妥株单抗

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Pertuzumab 是人源化单克隆抗体,是HER2二聚化抑制剂,可用于转移性 HER2 阳性乳腺癌的研究。
T6308 Stattic

STAT3 Inhibitor V

Apoptosis; STAT Apoptosis; JAK/STAT signaling; Stem Cells
Stattic (STAT3 Inhibitor V) 是一种 STAT3 抑制剂 (IC50=5.1 μM),选择性地抑制 STAT3 活化、二聚化和核转位。Stattic 具有抗肿瘤活性,可诱导细胞凋亡。
T9908 Pembrolizumab

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
Pembrolizumab 是一种抑制 PD-1 受体的人源化单克隆抗体,是一个 HER2 二聚化抑制剂类,它会削弱 HER2 与 HER 家族其他成员结合的能力。
T14091 AC-73

Autophagy Autophagy
AC-73 是一种可口服的 Cluster of Differentiation 147 (CD147) 抑制剂,具有很高的生物利用,可选择性破坏 CD147 的二聚化 (结合位点在 CD147 的 N 端 IgC2 域中包括 Glu64 和 Glu73),从而对 CD147/ERK1/2/STAT3/MMP-2 途径产生抑制,并抑制肝癌细胞的运动和侵袭。AC-73 具有抗增殖活性,诱导白血病细胞自噬。
T76776 Emactuzumab

RO 5509554,RG 7155

c-Fms; TAM Receptor Tyrosine Kinase/Adaptors
Emactuzumab(RG 7155) 是一种针对集落刺激因子-1 受体的单克隆抗体,靶向肿瘤相关巨噬细胞 (TAM)。Emactuzumab 具有抗肿瘤活性,可抑制集落刺激因子 1 受体 (CSF1R) 的激活。Emactuzumab 对 CSF-1R 具有高亲和力,Ki 值为 0.2 nM。Emactuzumab 可阻断 CSF-1R 二聚化,可用于研究如弥漫型腱鞘巨细胞瘤(dt-GCT)类的癌症。
T61346 Ph-Ph+

Ph-Ph+ is a hemiprotonic compound derived from the dimerization of phenanthroline (ph). It exhibits remarkable antitumor, antibacterial, and antifungal properties [1].
T70726 RO2443

RO2443 is a dual inhibitor of the MDM2-p53 or MDMX-p53 protein-protein interaction, inducung MDM2 and MDMX dimerization and activating the p53 pathway.
T35159 XCT0135908

XCT 0135908,XCT-0135908

XCT0135908 is a selectivity agonist of RXR -Nurr1 over a broad range of other RXR dimerization partners but with a rather low potency.
T10291 α-Truxillic acid

Others Others
α-Truxillic acid is formed by the dimerization of two molecules of α-trans-cinnamic acid with anti-inflammatory activities.
T16937 ST 2825

Others Others
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
T39487 HaXS8

HaXS8 is a dimerizer that facilitates the covalent and irreversible intracellular dimerization of proteins of interest labeled with HaloTag and SNAP-tag. Furthermore, HaXS8 does not exhibit any interference with PI3K/mTOR signaling.
T76416 Yp537

Yp537 是雌激素受体 (ER) 抑制剂,可阻止人类雌激素受体的二聚。
T77926 PROTAC KRAS G12C degrader-1

PROTACs PROTAC
PROTACKRAS G12C degrader-1是基于Cereblon的KRASG12C PROTAC降解剂,能诱导CRBN/KRASG12C二聚化,并在报告细胞中降解GFP-KRASG12C。
T38372 2-Fluoro-4-iodo benzonitrile

2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypan...
T76417 Yp537 TFA

Yp537 TFA 是雌激素受体 (ER) 抑制剂,可阻止人类雌激素受体的二聚。
T71839 ATV399

ATV399 is an inhibitor of iNOS dimerization which protects against Cytokine-Induced rat β-cell dysfunction, thereby inhibiting cleaved caspase-9 activation and subsequent β-cell apoptosis induced by a combination of IL-1β, IFN-γ, and high glucose.
T82950 ATIC-IN-1

ATIC-IN-1 (compound 14) 是一种针对ATIC二聚体化的抑制剂,具有Ki值685 nM。ATIC二聚体形成对AICAR转化酶功能是必要的。ATIC-IN-1展现了通过减少细胞数和降低细胞分裂率的抗肿瘤活性。
T62229 BBS-4

BBS-4 是一种选择性的、有效的诱导型一氧化氮合酶 (NOS2) 二聚抑制剂 (IC50: 0.49 nM),BBS-4 能够保护小鼠,使其免受败血症的心血管功能障碍的影响。
TP2046 TAT-cyclo-CLLFVY

Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cance
T61929 PD-1/PD-L1-IN-14

PD-1/PD-L1-IN-14 (compound 17) 是PD-1/PD-L1相互作用的抑制剂(IC50= 27.8 nM)。通过抑制PD-1/PD-L1 相互作用,PD-1/PD-L1-IN-14促进二聚化,内吞作用并降解 PD-L1。
T35429 AC-4-130

AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ultimately leading to cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 exhibits notable anti-cancer properties and effectively suppresses abnormal STAT5 activity in acute myeloid leukemia (AML), making it a promising therapeutic option [1].
T77774 tetrathiomolybdate

Tetrathiomolybdate (TM) 通过其特征性硫桥Mo2S6O2簇促进细胞铜外排蛋白ATP7B的金属结合域(WLN4)二聚化,应用于威尔逊病(Wilson’s disease)的临床治疗。
T82890 bFGF (119-126)

bFGF (119-126) 为具备生物活性的肽段,对应人类、牛(119-126)、小鼠、大鼠(118-125)以及肝素结合生长因子2(118-125)的相应残基。该肽能够抑制bFGF受体的二聚化及其激活作用。
T78534 NVOC cage-TMP-Halo

Others Others
NVOC cage-TMP-Halo是一种具有细胞渗透能力和光激活特性的蛋白质二聚化诱导剂。该化合物可对活细胞内蛋白质定位进行快速且可逆的控制,适用于研究动态细胞过程。
T78159 ATIC-IN-1 acetate

Others Others
ATIC-IN-1 (compound 14) acetate 是针对氨基咪唑甲酰胺核糖核苷酸转化酶/肌苷一磷酸环化水解酶 (ATIC) 的抑制剂,其Ki值为685 nM。该化合物阻碍ATIC二聚体的形成,此过程对于其转化酶活性中氨基咪唑甲酰胺核糖核苷酸 (AICAR) 的催化至关重要。ATIC-IN-1 acetate 显示出降低细胞数量及细胞分裂率的抗肿瘤效果。
T38329 CU-76

CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP sy...
T63339 ALV1

ALV1 是 Ikaros 和 Helios 的有效降解剂,对 IKZF1/2/3 具有相似的降解活性。ALV1 可以明显减少 IKZF1-4、CK1α (酪蛋白激酶 1α,CSNK1A1) 和核糖体蛋白 RPL4 的蛋白丰度,并诱导 Helios/CRBN 二聚反应,促进了 IL-2 的分泌。
T38328 CU-32

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas...
T72721 PD-1/PD-L1-IN-29

PD-1/PD-L1-IN-29(S4-1),有效PD-1/PD-L1抑制剂,IC50值为6.1 nM。能够结合PD-L1,破坏PD-1/PD-L1相互作用,诱导PD-L1二聚化与内化,有助于改善其对内质网的定位并促进PD-L1进入内质网,展现出抗癌活性。
T83875 HUP-55

HUP-55是一种脯氨酸内肽酶的抑制剂(IC50 = 5 nM)。在10 µM的浓度下,它可减少Neuro2a细胞中α-突触核蛋白二聚体的形成,促使HEK293细胞发生自噬,并降低SH-SY5Y细胞中由过氧化氢诱导的反应性氧种(ROS)产量的增加。此外,HUP-55(10 mg/kg)在通过腺病毒递送α-突触核蛋白编码载体(AAV-αSyn)诱导的帕金森病小鼠模型中,能减少患侧爪的使用和纹状体中寡聚体α-突触核蛋白水平。

化合物

LQZ-7I
Cat.No: T8469
Synonym:
Target: Survivin
BMS-1166
Cat.No: T5697
Synonym:
Target: PD-1/PD-L1
Mycro 3
Cat.No: T4367
Synonym: Mycro-3
Target: c-Myc, Autophagy
10074-G5
Cat.No: T3686
Synonym:
Target: c-Myc, Autophagy
TFIIH Modulator-19
Cat.No: T21083
Synonym: TFIIH Modulator19,TFIIH Modulator 19
Target: Others
VRT-325
Cat.No: T35074
Synonym: CFcor 325,VRT-534,CFcor325,VRT 325,VRT325,CF-106951,CFcor-325
Target: Others
2,5-Dihydroxybiphenyl
Cat.No: T21082
Synonym: TFIIH Modulator 12,2,5-二羟基联苯,TFIIH Modulator12
Target: Others
DEL-22379
Cat.No: T6818
Synonym: DEL22379
Target: Apoptosis, ERK
Firsocostat
Cat.No: T7184
Synonym: ND-630,NDI-010976,GS-0976
Target: Acetyl-CoA Carboxylase
STX-0119
Cat.No: T60160
Synonym:
Target: STAT
NSC 228155
Cat.No: T6908
Synonym: NSC228155
Target: EGFR, Epigenetic Reader Domain, DNA/RNA Synthesis, Histone Acetyltransferase
Pertuzumab
Cat.No: T9909
Synonym: 帕妥珠单抗,帕妥株单抗
Target: EGFR
Stattic
Cat.No: T6308
Synonym: STAT3 Inhibitor V
Target: Apoptosis, STAT
Pembrolizumab
Cat.No: T9908
Synonym:
Target: PD-1/PD-L1
AC-73
Cat.No: T14091
Synonym:
Target: Autophagy
Emactuzumab
Cat.No: T76776
Synonym: RO 5509554,RG 7155
Target: c-Fms, TAM Receptor
Ph-Ph+
Cat.No: T61346
Synonym:
Target:
RO2443
Cat.No: T70726
Synonym:
Target:
XCT0135908
Cat.No: T35159
Synonym: XCT 0135908,XCT-0135908
Target:
α-Truxillic acid
Cat.No: T10291
Synonym:
Target: Others
ST 2825
Cat.No: T16937
Synonym:
Target: Others
HaXS8
Cat.No: T39487
Synonym:
Target:
Yp537
Cat.No: T76416
Synonym:
Target:
PROTAC KRAS G12C degrader-1
Cat.No: T77926
Synonym:
Target: PROTACs
2-Fluoro-4-iodo benzonitrile
Cat.No: T38372
Synonym:
Target:
Yp537 TFA
Cat.No: T76417
Synonym:
Target:
ATV399
Cat.No: T71839
Synonym:
Target:
ATIC-IN-1
Cat.No: T82950
Synonym:
Target:
BBS-4
Cat.No: T62229
Synonym:
Target:
TAT-cyclo-CLLFVY
Cat.No: TP2046
Synonym:
Target:
PD-1/PD-L1-IN-14
Cat.No: T61929
Synonym:
Target:
AC-4-130
Cat.No: T35429
Synonym:
Target:
tetrathiomolybdate
Cat.No: T77774
Synonym:
Target:
bFGF (119-126)
Cat.No: T82890
Synonym:
Target:
NVOC cage-TMP-Halo
Cat.No: T78534
Synonym:
Target: Others
ATIC-IN-1 acetate
Cat.No: T78159
Synonym:
Target: Others
CU-76
Cat.No: T38329
Synonym:
Target:
ALV1
Cat.No: T63339
Synonym:
Target:
CU-32
Cat.No: T38328
Synonym:
Target:
PD-1/PD-L1-IN-29
Cat.No: T72721
Synonym:
Target:
HUP-55
Cat.No: T83875
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6995 Ochromycinone

STA 21,STA21,STA-21

Antibacterial; STAT JAK/STAT signaling; Microbiology/Virology; Stem Cells
Ochromycinone (STA 21) 是一种天然抗生素,也是一种 STAT3抑制剂。它可抑制 STAT3DNA 结合活性,STAT3二聚化。它具有抗癌和抗菌活性。
T38108 Fulvic Acid

Antioxidant; PDE Metabolism; oxidation-reduction
Fulvic Acid 是一种来自土壤、沉积物或水生环境中微生物产生的腐殖质的天然产物,是一种首次青霉菌中分离出的酚酸和真菌代谢产物。Fulvic Acid 抑制淀粉样蛋白b (17-42) (AB17-42)二聚化,破坏预先形成的AB17-42三聚体,并结合到磷酸二酯酶5A (PDE5A)的催化位点,可以调节机体免疫系统,影响细胞的氧化状态,改善胃肠功能。Fulvic Acid 可作为氧化剂或还原剂, 具有研究糖尿病等慢性炎症性疾病的潜力。
TN2767 2'-Hydroxygenistein

鲁冰花

Antifection Microbiology/Virology
2'-Hydroxygenistein has antifungal activity, dimerization of it causes a remarkable increase of antifungal activity. It shows significant concentration-dependent inhibitory effects on the release of beta-glucuronidase and lysozyme from rat neutrophils in response to formyl-Met-Leu-Phe/cytochalasin B. 2'-Hydroxygenistein of genistein can enhance its antioxidant activity and cell cytotoxicity in MCF-7 human breast cancer cells.

天然产物

Ochromycinone
Cat.No: T6995
Synonym: STA 21,STA21,STA-21
Target: Antibacterial, STAT
Fulvic Acid
Cat.No: T38108
Synonym:
Target: Antioxidant, PDE
2'-Hydroxygenistein
Cat.No: TN2767
Synonym: 鲁冰花
Target: Antifection
TargetMol Loading
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