2738
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5835 |
PROTAC ERRα ligand 2
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
PROTAC ERRα ligand 2 是雌激素相关受体 α (ERRα)反向激动剂。它对 ERRα (IC50=5.67 nM) 的抑制作用比 XCT790 (IC50=61.3 nM) 高效约 11 倍。 | |||
T15191 |
PROTAC ERRα ligand 1
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
PROTAC ERRα ligand 1 是一种雌激素相关受体 α (ERRα) 拮抗剂,能够作用于 ERRα (IC50:0.04 μM)和 ERRγ (IC50:2.8 μM)。 | |||
T5437 |
Gefitinib-based PROTAC 3
|
EGFR; PROTACs | Angiogenesis; JAK/STAT signaling; PROTAC; Tyrosine Kinase/Adaptors |
Gefitinib-based PROTAC 3 通过 linker 将 EGFR 结合元件与 von Hippel-Lindau 配体结合,在 HCC827(外显子 19 del)和 H3255(L858R 突变)细胞中诱导 EGFR 降解,DC50 分别为 11.7 和 22.3 nM。 | |||
T12551 |
PROTAC BRD4 ligand-1
|
Epigenetic Reader Domain; Ligands for Target Protein for PROTAC | Chromatin/Epigenetic; PROTAC |
PROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体,也是一种 BET 的抑制剂。 | |||
T13721 |
Homo-PROTAC cereblon degrader 1
|
Others; PROTACs | Others; PROTAC |
Homo-PROTAC cereblon degrader 1 (compound 15a) 是一种高效 cereblon 降解剂,对 IKZF1 和 IKZF3 的影响很小。 | |||
T13722 |
Homo-PROTAC pVHL30 degrader 1
|
Others; PROTACs | Others; PROTAC |
Homo-PROTAC pVHL30 degrader 1 是一种基于 PROTAC 的 pVHL30 降解剂。 | |||
T13848 |
SMARCA-BD ligand 1 for Protac
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
SMARCA-BD ligand 1 for Protac 能够与 BAF ATPase 亚基 SMARCA2 结合,可用于 PROTAC 技术,用于降解 SMARCA2。 | |||
T40112 |
PROTAC PD-1/PD-L1 degrader-1
|
PD-1/PD-L1; PROTACs | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; PROTAC |
PROTAC PD-1/PD-L1 degrader-1 是一种降解 PD-L1 的 PROTAC,抑制 PD-1/PD-L1 相互作用(IC50:39.2 nM)。PROTAC PD-1/PD-L1 degrader-1 可恢复 Hep3B/OS-8/hPD-L1 和 CD3 T 细胞共培养模型中被抑制的免疫力,可通过溶酶体依赖性方式降低 PD-L1 的蛋白质含量。 | |||
T13890 |
SMARCA-BD ligand 1 for Protac dihydrochloride
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
SMARCA-BD ligand 1 for Protac dihydrochloride 是一种能够与 BAF ATPase 亚基 SMARCA2 结合的化合物,基于 PROTAC 技术,使 SMARCA2 降解。 | |||
T74186 |
PROTAC-O4I2
|
Apoptosis; PROTACs | Apoptosis; PROTAC |
PROTAC-O4I2 是一种靶向剪接因子 3B1 (SF3B1) 的 PROTAC连接体, 在 K562 细胞中促使 FLAG-SF3B1 降解,IC50 值为 0.244 μM。PROTAC-O4I2 促使 K562 WT 细胞凋亡 (apoptosis)。 | |||
T34168 |
PROTAC-I
PROTAC I |
Others | Others |
PROTAC-I targets steroid hormone receptors for ubiquitination and degradation. | |||
T39997 |
PROTAC CDK9 ligand-1
PROTAC CDK9 ligand-1 |
Others | Others |
PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs. | |||
T40072 |
PROTAC BRD4 Degrader-9
PROTAC BRD4 Degrader-9 |
Others | Others |
PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound consisting of ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound can effectively degrade the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM. | |||
T37329 |
PROTAC IDO1 Degrader-1
PROTAC IDO1 Degrader-1 |
PROTACs | PROTAC |
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24... | |||
T18639 |
Cl-C6-PEG4-O-CH2COOH
PROTAC Linker 4 |
Others | Others |
Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) 是一种有效的基于聚乙二醇的 PROTAC 连接剂,常被用于 PROTAC 合成氯烷(HaloPROTACs)。 | |||
T36242 |
PROTAC BRD4 Degrader-5
PROTAC BRD4 Degrader-5 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines[1]. | |||
T39902 |
PROTAC IRAK4 degrader-5
PROTAC IRAK4 degrader-5 |
Others | Others |
PROTAC IRAK4 degrader-5 is a Cereblon-based IRAK4 degrader. | |||
T40073 |
PROTAC BRD4 Degrader-10
PROTAC BRD4 Degrader-10 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM. | |||
T40074 |
PROTAC BRD4 Degrader-15
PROTAC BRD4 Degrader-15 |
Others | Others |
PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2. Additionally, PROTAC BRD4 Degrader-15 demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells. | |||
T39920 |
PROTAC IRAK4 degrader-3
PROTAC IRAK4 degrader-3 |
PROTACs | PROTAC |
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau. | |||
T39628 |
PROTAC BRD4 ligand-2
PROTAC BRD4 ligand-2 |
Others | Others |
PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718. | |||
T39901 |
PROTAC IRAK4 degrader-4
PROTAC IRAK4 degrader-4 |
Others | Others |
PROTAC IRAK4 degrader-4 (US20190192668A1, compound I-127) is a Cereblon-based PROTAC specifically designed to target and degrade interleukin-1 receptor-associated kinase 4 (IRAK4). | |||
T40334 |
PROTAC IRAK3 degrade-1
PROTAC IRAK3 degrade-1 |
Others | Others |
PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 ( IC 50 = 5 nM). | |||
T36628 |
PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degra... | |||
T39903 |
PROTAC IRAK4 degrader-6
PROTAC IRAK4 degrader-6 |
Others | Others |
PROTAC IRAK4 degrader-6 is a potent Cereblon-based compound designed to degrade interleukin-1 receptor-associated kinase 4 (IRAK4). | |||
T40075 |
PROTAC BRD4 Degrader-13
PROTAC BRD4 Degrader-13 |
Others | Others |
PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (PROTAC), linking ligands for von Hippel-Lindau and BRD4 proteins. In the context of PC3 prostate cancer cells, this compound effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies. The degradation of BRD4 protein is achieved with remarkable potency, exhibiting a DC 50 of 0.025 nM and 6.0 nM when combined with STEAP1 and CLL1 antibodies, respectively. | |||
T39996 |
PROTAC CDK9 degrader-4
PROTAC CDK9 degrader-4 |
Others | Others |
PROTAC CDK9 degrader-4 is a potent and efficacious chemical compound designed specifically to degrade CDK9, a protein involved in transcription regulation. This compound effectively targets and reduces the levels of CDK9, thereby modulating transcriptional activity. | |||
T40143 |
PROTAC CBP/P300 Degrader-1
PROTAC CBP/P300 Degrader-1 |
PROTACs | PROTAC |
PROTAC CBP/P300 Degrader-1 is an effective compound that degrades CBP/P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines. | |||
T8745 |
PROTAC BRAF-V600E degrader-1
Compound 23 |
Raf; PROTACs | MAPK; PROTAC |
PROTAC BRAF-V600E degrader-1 (Compound 23) 选择性地诱导 BRAF-V600E 的降解,而不是野生型 BRAF。 | |||
T32043 |
HaloPROTAC3
Halo PROTAC-3,HaloPROTAC 3,HaloPROTAC-3 |
Ligand for E3 Ligase | PROTAC |
HaloPROTAC3 (HaloPROTAC-3) 是 E3 配体和 16 原子长度接头的偶联物,也是 HaloTag 融合蛋白的降解剂。 | |||
T18629 |
PEG3-O-CH2COOH
PROTAC Linker 8,三聚乙二醇-乙酸 |
Others; PROTAC Linker | Others; PROTAC |
PEG3-O-CH2COOH (PROTAC Linker 8) 是一种属于 PEG 类的 PROTAC linker,可用于 SNIPER 分子的合成。 | |||
T18595 |
Dasatinib carbaldehyde
PROTAC ABL binding moiety 4,BMS-354825 carbaldehyde |
Others; Ligands for Target Protein for PROTAC | Others; PROTAC |
Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) 基于 ABL 抑制剂达沙替尼,通过接头与 IAP 配体结合,形成 SNIPER [1]。 | |||
T18614 |
Bis-Tos-PEG4
Tetraethylene glycol di(p-toluenesulfonate),PROTAC Linker 16,1,11-Bis(tosyloxy)-3,6,9-trioxaundecane |
Others; PROTAC Linker | Others; PROTAC |
Bis-Tos-PEG4 (PROTAC Linker 16) 是一种属于 PEG 类的 PROTAC linker,可用于 PROTAC 分子的合成。 | |||
T36256 |
LC-2
LC 2,PROTAC KRASG12C Degrader-LC-2,LC2 |
PROTACs | PROTAC |
LC-2 (PROTAC KRASG12C Degrader-LC-2) 是一种新型基于von Hippel-Lindau的内源性 KRAS G12C 的 PROTAC 降解剂,DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VH的 PROTAC,诱导 KRAS G12C 快速持续降解。LC-2 对纯合和杂合子 KRAS G12C 细胞系 MAPK 信号有抑制作用。 | |||
T18616 |
NH2-C2-NH-Boc
PROTAC Linker 22,N-叔丁氧羰基-1,2-乙二胺 |
Others; PROTAC Linker | Others; PROTAC |
NH2-C2-NH-Boc (PROTAC Linker 22) 是一种属于 alkyl chain 类的 PROTAC linker,可用于 PROTAC 分子的合成。 | |||
T39837 |
PROTAC ERRα Degrader-3
|
PROTACs | PROTAC |
PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins. | |||
T36243 |
PROTAC RIPK degrader-6
|
PROTACs | PROTAC |
PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker to a cereblon binder[1]. | |||
T18617 |
NH2-C5-NH-Boc
N-(5-氨基戊基)氨基甲酸叔丁酯,PROTAC Linker 23 |
Others; PROTAC Linker | Others; PROTAC |
NH2-C5-NH-Boc (PROTAC Linker 23) 是一种属于 alkyl chain 类的 PROTAC linker,可用于 PROTAC 分子的合成。 | |||
T13847 |
PROTAC SGK3 degrader-1
SGK3-PROTAC1 |
SGK; PROTACs | Metabolism; PROTAC |
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种靶向 SGK3 且与 VH032 VHL 结合配体的 PROTAC 偶联物,可诱导内源性 SGK3 降解。PROTAC SGK3 degrader-1 可抑制GDC0941诱导的癌细胞增殖。 | |||
T7701 |
Boc-NH-PEG3
PROTAC Linker 10,2-[2-(2-T-BOC-氨基乙氧基)乙氧基]乙醇 |
Others; PROTAC Linker | Others; PROTAC |
Boc-NH-PEG3 (PROTAC Linker 10) 是一种属于 PEG 类的 PROTAC linker,可用于 PROTAC 的合成分子。 | |||
T83857 |
Soluble Epoxide Hydrolase PROTAC 1a
sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a |
Others | Others |
Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术,通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解,特异性抑制sEH的水解酶活性(IC50 = 0.8 nM),相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解,并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接,表明能减少ER应激。 | |||
T39374 |
PROTAC BET Degrader-10
|
PROTACs | PROTAC |
PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM. | |||
T13915L |
PROTAC BRD9-binding moiety 1 hydrochloride
PROTAC BRD9-binding moiety 1 hydrochloride (2097512-23-5 free base) |
Others | Others |
PROTAC BRD9-binding moiety 1 hydrochloride binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC. | |||
T17995 |
Halo PROTAC 1
|
Others | Others |
Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker[1]. | |||
T41267 |
PROTAC(H-PGDS)-7
|
Others | Others |
PROTAC(H-PGDS)-7 是一种有选择性的、有效的小分子造血前列腺素 D 合酶 (H-PGDS)PROTAC 降解剂,在 KU812细胞中展现出降解活性,DC50为 17.3 pM。PROTAC(H-PGDS)-7是一种类药化合物,能有效抑制前列腺素 D2 (PGD2)的产生,抑制炎症因子重生作用。PROTAC(H-PGDS)-7是治疗 DMD 和其他H-PGDS 相关疾病的候选化合物。 | |||
T13845 |
PROTAC PARP1 degrader
|
Others | Others |
PROTAC PARP1 degrader is a degrader of PARP1 based on the PROTAC technology. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line (IC50 of 6.12 μM). | |||
T5438 |
PROTAC CDK9 Degrader-1
|
CDK; PROTACs | Cell Cycle/Checkpoint; PROTAC |
PROTAC CDK9 Degrader-1 是一种选择性 CDK9 降解剂,是由Cereblon 配体和CDK 配体相连的PROTAC。 | |||
T36247 |
TBK1 control PROTAC® 4
|
Others | Others |
Negative control for TBK1 PROTAC 3i. Binds TBK1 with high affinity, but exhibits no significant degradation of TBK1. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license. | |||
T13694 |
FKBP12 PROTAC RC32
RC32 |
Others; PROTACs | Others; PROTAC |
FKBP12 PROTAC RC32 contains conjugation of Rapamycin and a ligand for an E3 ubiquitin ligase.FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. | |||
T18634 |
PROTAC MDM2 Degrader-4
|
Others | Others |
PROTAC MDM2 Degrader-4 is a compound designed using PROTAC technology to degrade MDM2. It combines a powerful MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9784 |
Docosanedioic acid
|
PROTAC Linker; ADC Linker | Antibody-drug Conjugate/ADC Related; PROTAC |
Docosanedioic acid 可以作为ADC linker 或PROTAC linker,用于合成抗体偶联药物或合成 PROTAC。 |