147
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T18064 |
Lenalidomide-Br
|
Ligand for E3 Ligase | PROTAC |
Lenalidomide-Br (Compound 41) is a derivative of Lenalidomide, which serves as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound, Lenalidomide-Br, can be conjugated to a protein ligand through a linker to create PROTACs. For instance, Lenalidomide-Br is utilized as a component in the PROTAC STAT3 degrader SD-36. | |||
T21938 |
AS-041164
|
PI3K | PI3K/Akt/mTOR signaling |
AS-041164 是选择性的,具有口服活性的PI3Kγ亚型抑制剂,IC50=70 nM。它对 PI3Kα (IC50:240 μM),PI3Kβ (IC50:1.45 μM) 和 PI3Kδ (IC50:1.70 μM) 的活性较低。它具有抗炎活性。 | |||
T40548 |
NH-3
|
Thyroid hormone receptor(THR) | Endocrinology/Hormones |
NH-3 is a potent orally active thyroid hormone receptor (THR) antagonist which exhibits reversible behavior, demonstrated by an IC 50 of 55 nM. Derived from the selective thyromi-metic GC-1, NH-3 effectively inhibits the binding of thyroid hormones to their respective receptors, resulting in hindered cofactor recruitment. | |||
T28073 |
MLS1547
MLS000051547,MLS 1547,MLS-1547 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂,Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导,EC50 为 0.37 μM。 | |||
T26869 |
BMS-986122
BMS 986122 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BMS-986122 (BMS 986122) 是选择性 μ 阿片受体正变构调节剂,可增加 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的作用,还增强 DAMGO 介导的 [35S]GTPγS 在小鼠脑膜中的结合。 | |||
T8497 |
SX-682
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂,可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫,具有治疗去势抵抗性前列腺癌的潜力。 | |||
T16850 |
SB-265610
GSK-CXCR2 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SB-265610 (GSK-CXCR2) 是竞争性非肽变构CXCR2选择性拮抗剂,可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50分别为 3.7 和 70 nM。 | |||
T4657 |
WHI-P97
4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉 |
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
WHI-P97 是一种选择性 JAK-3抑制剂,可用于预防过敏性哮喘的研究。 | |||
T14667 |
BLT-1
|
Others; HCV Protease | Microbiology/Virology; Others; Proteases/Proteasome |
BLT-1 是一种氨基硫脲铜螯合剂,是一种选择性清除受体 B1 型 (SR-BI) 抑制剂,抑制高密度脂蛋白 (HDL) 和 SR-BI 介导的细胞之间的脂质转移。 | |||
T40028 |
(S,R,S)-AHPC
|
Ligand for E3 Ligase | PROTAC |
(S,R,S)-AHPC 是一种 VHL 配体,用于募集 VHL 蛋白。 | |||
T40503 |
Thalidomide-5-methyl
|
Ligand for E3 Ligase | PROTAC |
Thalidomide-5-methyl 是基于 Thalidomide 的 CRBN 配体,可以用于CRBN 的招募。 | |||
T18831 |
Thalidomide-propargyl
|
Others; Ligand for E3 Ligase | Others; PROTAC |
Thalidomide-propargyl 是一种基于 Thalidomide 的 Cereblon 配体,可用于募集 CRBN 蛋白。它能够利用 linker 与靶蛋白配体连接,得到含 IMiD 的 PROTAC。 | |||
T22021 |
ACHP
IKK-2 Inhibitor VIII |
IκB/IKK | NF-κB |
ACHP(IKK-2 Inhibitor VIII) 是一种新型具有选择性和高效性的 IKK 抑制剂,对IKK-α和IKK-β 具有抑制作用。ACHP 具有抗 HIV-1 活性,通过抑制 NF-κB 激活来抑制 HIV-1 长末端重复序列 (LTR) 驱动的基因表达,抑制 TNF-α 诱导的 NF-κB (p65)募集到 HIV-1 LTR。 | |||
T7329 |
C-178
|
STING | Immunology/Inflammation |
C-178 是 STING 选择性共价抑制剂,与 Cys91 结合抑制小鼠中由不同的激活剂引起的 STING 反应。 | |||
T9029 |
STING-IN-3
C-171 |
STING | Immunology/Inflammation |
STING-IN-3 (C-171) 是干扰素基因刺激物 (STING) 的抑制剂。 它与 STING 结合,抑制其棕榈酰化,并阻止 TBK1 的募集和磷酸化。 | |||
TP1922L1 |
ELA-11 (human) acetate(1784687-32-6 free base)
|
Apelin receptor; Arrestin | GPCR/G Protein |
ELA-11 (human) acetate(1784687-32-6 free base)是亲和力 apelin 受体激动剂 (Ki = 14 nM)。 ELA-32 的生物活性片段。在体外抑制毛喉素诱导的 cAMP 产生并刺激 β-arrestin 募集。 | |||
T18066 |
Lenalidomide-OH
|
Ligand for E3 Ligase | PROTAC |
Lenalidomide-OH is a ligand of cereblon (CRBN), serving as an analog to Lenalidomide for E3 ubiquitin ligase. It is utilized in the recruitment of CRBN protein. Additionally, Lenalidomide-OH can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. An example of a PROTAC BTK degrader incorporating Lenalidomide-OH is SJF620. | |||
T7753 |
Thalidomide-O-COOH
Cereblon ligand 3,E3 ligase Ligand 3,TCE35031 |
Others; Ligand for E3 Ligase | Others; PROTAC |
Thalidomide-O-COOH (Cereblon ligand 3) 是一种基于 Thalidomide 的 Cereblon 配体,可用于募集 CRBN 蛋白。它能够利用 linker 与靶蛋白配体连接,得到 PROTAC 分子。 | |||
T9291 |
Thalidomide-5-OH
4 - 羟基沙利度胺,2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione |
Others; Ligand for E3 Ligase | Others; PROTAC |
Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) 是基于 Thalidomide 的的cereblon 配体,可用于募集CRBN 蛋白。它能够利用 linker 与靶蛋白配体连接,得到 PROTAC 分子。 | |||
T39988 |
6'-GNTI dihydrochloride
|
Opioid Receptor; Akt | Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; PI3K/Akt/mTOR signaling |
6'-GNTI dihydrochloride 是一种κ-阿片受体(KOR)激动剂,它偏向于激活 G 蛋白介导的信号传导,而不是β-阿司匹林2的募集。6'-GNTI dihydrochloride 只能激活纹状体神经元中的 Akt 通路。 | |||
T77673 |
7-FluorotryptaMine HCl
|
GPR; Arrestin | Endocrinology/Hormones; GPCR/G Protein |
7-FluorotryptaMine HCl 是一种有效的芳香单胺 GPRC5A 激动剂,可诱导 GPRC5A 介导的 β-arrestin 募集。7-FluorotryptaMine HCl 可用于研究与免疫和癌症相关的信号通路。 | |||
T13671 |
(S,R,S)-AHPC-Me hydrochloride
VHL ligand 2 hydrochloride,E3 ligase Ligand 1 |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein. | |||
T8412 |
(S,R,S)-AHPC
VH032-NH2,MDK7526,VHL ligand 1 |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC (VH032-NH2) 是一种 VH032-based VHL ligand,可用于募集 von Hippel-Lindau (VHL)蛋白。它能够利用 linker 与靶蛋白配体连接,得到 PROTAC 分子。 | |||
T76882 |
Talquetamab
JNJ-64407564,JNJ-7564 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Talquetamab (JNJ-64407564)是一种用于多发性骨髓瘤的 T 细胞重定向 GPRC5D 双特异性抗体,具有抗肿瘤活性,通过T 细胞的募集和活化诱导 T 细胞介导的杀死表达 GPRC5 的 MM 细胞。Talquetamab 可用于治疗多发性骨髓瘤 (MM)。 | |||
T13877 |
(S,S,S)-AHPC hydrochloride
(S,S,S)-VH032-NH2 hydrochloride,(S,S,S)-AHPC盐酸盐 |
Ligand for E3 Ligase | PROTAC |
(S,S,S)-AHPC hydrochloride ((S,S,S)-VH032-NH2 hydrochloride) 是 von Hippel-Lindau (VHL) 氨基砌块。(S,S,S)-AHPC (Compound 27) 常作为 (S,R,S)-AHPC 的阴性对照。(S,R,S)-AHPC 是基于 VH032 的 VHL 配体,可用于募集 VHL 蛋白。 | |||
T7755 |
Thalidomide 4-fluoride
E3 ligase Ligand 4,2-(2,6-二氧代-哌啶-3-基)-4-氟基-异吲哚-1,3-二酮 |
IRAK; Ligand for E3 Ligase | Immunology/Inflammation; NF-κB; PROTAC |
Thalidomide 4-fluoride (E3 ligase Ligand 4) 是一种基于 Thalidomide 的 Cereblon 配体,可用于募集 CRBN 蛋白。它能够利用 linker 与 IRAK4 靶蛋白配体连接,得到 PROTAC IRAK4 degrader-1。 | |||
T15611 |
JH-RE-06
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
JH-RE-06是一种REV1-REV7互作抑制剂,IC50为0.78 μM,Kd 为0.42 μM。它靶向与 POLζ 的 REV7 亚基相互作用的 REV1,可改善化疗效果。它通过阻止诱变 POLζ 的募集来破坏诱变性跨损伤合成。 | |||
T17157 |
TRAF-STOP inhibitor 6877002
CD40-TRAF6 inhibitor |
NF-κB | NF-κB |
TRAF-STOP inhibitor 6877002 (CD40-TRAF6 inhibitor)是一种 CD40-TRAF6 相互作用的选择性抑制剂,可以抑制 RAW 细胞中 NF-κB 活化。TRAF-STOP 6877002 可阻止小鼠动脉粥样硬化的恶化,减少白细胞募集和巨噬细胞的活化,减少动脉粥样硬化斑块中的巨噬细胞增殖。 | |||
T17927 |
(S,R,S)-AHPC TFA
VH032-NH2 TFA,VHL ligand 1 TFA |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC TFA (VHL ligand 1 TFA) 是一种 VH032-based VHL ligand,可用于募集 von Hippel-Lindau (VHL)蛋白。它能够利用 linker 与靶蛋白配体连接,形成 PROTAC 分子。 | |||
T7752 |
(S,R,S)-AHPC-Me
VHL ligand 2,E3 ligase Ligand 1A |
Ligand for E3 Ligase | PROTAC |
(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) 是基于 (S,R,S)-AHPC 的的 VHL 配体,可用于募集 von Hippel-Lindau (VHL) 蛋白。它可有效降解去势抵抗性前列腺癌细胞中的 BET 蛋白,DC50<1 nM。它可用于合成 ARV-771。 | |||
T41231 |
GP 1a
|
Cannabinoid Receptor; PERK; Arrestin | Apoptosis; GPCR/G Protein |
GP 1a 是cannabinoid receptor 2(CB2)的强效激动剂(EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍,且在体外增加HL-60细胞的P-ERK1/2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成,同时促进上皮的重新形成。 | |||
T41068 |
P53R3
|
p53 | Apoptosis |
P53R3是一种有效的 p53再激活剂。P53R3可恢复 p53热点突变体的序列特异性 DNA 结合,包括p53 R175H、p53 R248W 和p53 R273H。P53R3特异性诱导p53依赖性抗增殖作用,其特异性比PRIMA-1高得多的。P53R3增强野生型p53和p53 M237I 向靶基因启动子的募集。P53R3强烈增强死亡受体死亡受体5(DR5)的mRNA、总蛋白和细胞表面的水平。P53R3用于癌症研究。 | |||
T63790 |
Cbl-b-IN-3
|
E1/E2/E3 Enzyme | Ubiquitination |
Cbl-b-IN-3是一种有效的casitas b 系淋巴瘤原癌基因-b (Cbl-b)抑制剂(ic50 < 1 nM)。Cbl-b 是一种环型E3泛素蛋白连接酶,与T 淋巴细胞激活阈值的设定有关。Cbl-b 以不依赖于蛋白水解的方式负调控p85,通过其E3泛素连接酶活性,参与了p85向CD28和T 细胞抗原受体ζ的募集,抑制PI3K 抑制了Cblb-/- t 细胞活化的增强。 | |||
T77579 |
JC2-11
|
IL Receptor; Dehydrogenase; ROS; Caspase; NOD-like Receptor (NLR); AIM2 | Apoptosis; Immunology/Inflammation; Metabolism; Proteases/Proteasome |
JC2-11 是一种对炎症有抑制作用的化合物。JC2-11 对含有募集结构域的蛋白质 NLRC 4、黑色素瘤 2 中缺失 (AIM 2) 和非典型 (NC) 炎症小体有抑制作用,通过破坏活性氧的产生和 caspase-1 的活性来抑制炎症小体的活化。JC2-11 减少了炎症小体中 caspase-1 (p20) 的分泌、gasdermin D (GSDMD) 的裂解、IL-1β 和乳酸脱氢酶 (LDH) 的释放。 | |||
T10926L | CYT-1010 hydrochloride | Others | Others |
CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively. | |||
T10926 | CYT-1010 | Others | Others |
CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively. | |||
T77951 |
Thalidomide-5-O-C4-NH2 hydrochloride
|
||
Thalidomide-5-O-C4-NH2 hydrochloride为一种Thalidomide衍生的cereblon配体,能够招募CRBN蛋白。它能通过linker与目标蛋白配体结合,进而构建PROTAC分子,如THAL-SNS-032。 | |||
T39721 |
Thalidomide-5-PEG2-Cl
Thalidomide-5-PEG2-Cl |
||
Thalidomide-5-PEG2-Cl, a Thalidomide-derived cereblon ligand, serves as the ligand for the recruitment of CRBN protein. It can be conjugated to the protein ligand via a linker to produce PROTACs. | |||
T40283 |
Thalidomide-5,6-Cl
|
||
Thalidomide-5,6-Cl, a derivative of Thalidomide, serves as a cereblon ligand for the recruitment of CRBN protein. It can be linked to a ligand for protein using a linker to form PROTACs. | |||
T14777 |
BRD5529
|
Others | Others |
BRD5529 is a selective inhibitor of CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction (IC50: 8.6 μM). BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation, and activation of CARD9. | |||
T70983 | Zoledronate disodium | ||
Zoledronate disodium is an inhibitor of osteoclastogenesis and macrophage recruitment, decreasing bone turnover and stabilizing the bone matrix, exhibiting diverse anti-tumor effects in osteosarcoma. | |||
T39032 |
Pomalidomide-5-O-CH3
Pomalidomide-5-O-CH3 |
||
Pomalidomide-5-O-CH3, a derivative of Pomalidomide, serves as a specific ligand for cereblon (CRBN) protein recruitment. It can be linked to the protein ligand to create a PROTAC. | |||
T71869 | IMB-10 | ||
IMB-10 is an alphaMbeta2 integrin modulator, inhibiting leukocyte migration and recruitment in vitro and in vivo. | |||
T39894 |
Thalidomide-4-C3-NH2 hydrochloride
Thalidomide-4-C3-NH2 hydrochloride |
||
Thalidomide-4-C3-NH2 hydrochloride is a Thalidomide-derived cereblon ligand utilized for the recruitment of CRBN protein. This compound can be linked to the ligand for protein using a linker to create PROTACs. | |||
T38457 |
Lenalidomide-4-OH
|
||
Lenalidomide-4-OH is a cereblon (CRBN) ligand derived from Lenalidomide, utilized in the recruitment of the CRBN protein. It can be conjugated to the protein ligand via a linker, facilitating the formation of PROTAC. | |||
T39699 |
Thalidomide-O-C8-Boc
Thalidomide-O-C8-Boc |
||
Thalidomide-O-C8-Boc is a Cereblon ligand derived from Thalidomide, primarily employed in the recruitment of CRBN protein. This ligand can be linked to a protein ligand via a linker to create PROTACs. | |||
T77960 |
Thalidomide-5-O-C13-NH2 hydrochloride
|
||
Thalidomide-5-O-C13-NH2 hydrochloride 是一款Thalidomide衍生的cereblon配体,能够招募CRBN蛋白。该化合物能通过linker与特定的靶蛋白配体结合,进而构建PROTAC分子,如THAL-SNS-032。 | |||
T40897 |
Lenalidomide-4-aminomethyl
|
||
Lenalidomide-4-aminomethyl is a CRBN ligand derived from Lenalidomide, which is utilized for the recruitment of CRBN protein. By linking Lenalidomide-4-aminomethyl to the ligand, a PROTAC can be formed. | |||
T39599 |
Lenalidomide-C5-amido-Boc
Lenalidomide-C5-amido-Boc |
||
Lenalidomide-C5-amido-Boc is a Cereblon ligand derived from Lenalidomide, and serves in the recruitment of CRBN protein. It can be effectively linked to the protein ligand through a linker, resulting in the formation of PROTAC. | |||
T61371 | CB1R Allosteric modulator 4 | ||
CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4953 |
Neotuberostemonine
|
NOS | Immunology/Inflammation |
Neotuberostemonine 是一种结核分枝杆菌根中主要的止咳生物碱,能够阻碍巨噬细胞的募集和活化,从而减轻博来霉素 (Bleomycin) 诱导的肺纤维化。 | |||
TN6458 |
Acetylshikonin
|
||
Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity. |