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2721

抑制剂 & 化合物

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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	Angiogenesis; JAK/STAT signaling; 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; Ligand for E3 Ligase	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; Ligand for E3 Ligase	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。
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。
T34168	PROTAC-I PROTAC I
	PROTAC-I targets steroid hormone receptors for ubiquitination and degradation.
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)。
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)。
T39997	PROTAC CDK9 ligand-1 PROTAC CDK9 ligand-1
	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
	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
	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...
T36242	PROTAC BRD4 Degrader-5 PROTAC BRD4 Degrader-5
	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].
T40073	PROTAC BRD4 Degrader-10 PROTAC BRD4 Degrader-10
	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.
T39902	PROTAC IRAK4 degrader-5 PROTAC IRAK4 degrader-5
	PROTAC IRAK4 degrader-5 is a Cereblon-based IRAK4 degrader.
T40074	PROTAC BRD4 Degrader-15 PROTAC BRD4 Degrader-15
	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.
T39628	PROTAC BRD4 ligand-2 PROTAC BRD4 ligand-2
	PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.
T39920	PROTAC IRAK4 degrader-3 PROTAC IRAK4 degrader-3
	PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
T39901	PROTAC IRAK4 degrader-4 PROTAC IRAK4 degrader-4
	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
	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
	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
	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
	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
	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
	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	MAPK
	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]。
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。
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。
T40112	PROTAC PD-1/PD-L1 degrader-1 PROTAC PD-1/PD-L1 degrader-1
	PROTAC PD-1/PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1/PD-L1 PROTAC that effectively inhibits the interaction between PD-1 and PD-L1 with an IC50 value of 39.2 nM. It successfully restores the suppressed immune response in a co-culture model consisting of Hep3B/OS-8/hPD-L1 cells and CD3 T cells. Additionally, this compound moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.
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
	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.
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。
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	Metabolism
	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。
T36243	PROTAC RIPK degrader-6
	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].
T39374	PROTAC BET Degrader-10
	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.
T83857	Soluble Epoxide Hydrolase PROTAC 1a sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a
	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。
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
	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).
T36247	TBK1 control PROTAC® 4
	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.
T5438	PROTAC CDK9 Degrader-1	CDK	Cell Cycle/Checkpoint
	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。
T13694	FKBP12 PROTAC RC32 RC32	Others	Others
	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].

化合物

PROTAC ERRα ligand 2

Cat.No: T5835

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

PROTAC ERRα ligand 1

Cat.No: T15191

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Gefitinib-based PROTAC 3

Cat.No: T5437

Target: EGFR

PROTAC BRD4 ligand-1

Cat.No: T12551

Target: Epigenetic Reader Domain, Ligands for Target Protein for PROTAC

Homo-PROTAC cereblon degrader 1

Cat.No: T13721

Target: Others, Ligand for E3 Ligase

Homo-PROTAC pVHL30 degrader 1

Cat.No: T13722

Target: Others, Ligand for E3 Ligase

SMARCA-BD ligand 1 for Protac

Cat.No: T13848

Target: Epigenetic Reader Domain

SMARCA-BD ligand 1 for Protac dihydrochloride

Cat.No: T13890

Target: Epigenetic Reader Domain

Cat.No: T34168

Synonym: PROTAC I

Cat.No: T74186

Target: Apoptosis, PROTACs

Cl-C6-PEG4-O-CH2COOH

Cat.No: T18639

Synonym: PROTAC Linker 4

Target: Others

PROTAC CDK9 ligand-1

Cat.No: T39997

Synonym: PROTAC CDK9 ligand-1

PROTAC BRD4 Degrader-9

Cat.No: T40072

Synonym: PROTAC BRD4 Degrader-9

PROTAC IDO1 Degrader-1

Cat.No: T37329

Synonym: PROTAC IDO1 Degrader-1

PROTAC BRD4 Degrader-5

Cat.No: T36242

Synonym: PROTAC BRD4 Degrader-5

PROTAC BRD4 Degrader-10

Cat.No: T40073

Synonym: PROTAC BRD4 Degrader-10

PROTAC IRAK4 degrader-5

Cat.No: T39902

Synonym: PROTAC IRAK4 degrader-5

PROTAC BRD4 Degrader-15

Cat.No: T40074

Synonym: PROTAC BRD4 Degrader-15

PROTAC BRD4 ligand-2

Cat.No: T39628

Synonym: PROTAC BRD4 ligand-2

PROTAC IRAK4 degrader-3

Cat.No: T39920

Synonym: PROTAC IRAK4 degrader-3

PROTAC IRAK4 degrader-4

Cat.No: T39901

Synonym: PROTAC IRAK4 degrader-4

PROTAC IRAK3 degrade-1

Cat.No: T40334

Synonym: PROTAC IRAK3 degrade-1

PROTAC BRD4 Degrader-8

Cat.No: T36628

Synonym: PROTAC BRD4 Degrader-8

PROTAC IRAK4 degrader-6

Cat.No: T39903

Synonym: PROTAC IRAK4 degrader-6

PROTAC BRD4 Degrader-13

Cat.No: T40075

Synonym: PROTAC BRD4 Degrader-13

PROTAC CDK9 degrader-4

Cat.No: T39996

Synonym: PROTAC CDK9 degrader-4

PROTAC CBP/P300 Degrader-1

Cat.No: T40143

Synonym: PROTAC CBP/P300 Degrader-1

PROTAC BRAF-V600E degrader-1

Cat.No: T8745

Synonym: Compound 23

Target: Raf

Cat.No: T32043

Synonym: Halo PROTAC-3,HaloPROTAC 3,HaloPROTAC-3

Target: Ligand for E3 Ligase

Cat.No: T18629

Synonym: PROTAC Linker 8,三聚乙二醇-乙酸

Target: Others, PROTAC Linker

Dasatinib carbaldehyde

Cat.No: T18595

Synonym: PROTAC ABL binding moiety 4,BMS-354825 carbaldehyde

Target: Others, Ligands for Target Protein for PROTAC

Cat.No: T36256

Synonym: LC 2,PROTAC KRASG12C Degrader-LC-2,LC2

Target: PROTACs

Cat.No: T18614

Synonym: Tetraethylene glycol di(p-toluenesulfonate),PROTAC Linker 16,1,11-Bis(tosyloxy)-3,6,9-trioxaundecane

Target: Others, PROTAC Linker

PROTAC PD-1/PD-L1 degrader-1

Cat.No: T40112

Synonym: PROTAC PD-1/PD-L1 degrader-1

Cat.No: T18616

Synonym: PROTAC Linker 22,N-叔丁氧羰基-1,2-乙二胺

Target: Others, PROTAC Linker

PROTAC ERRα Degrader-3

Cat.No: T39837

Cat.No: T7701

Synonym: PROTAC Linker 10,2-[2-(2-T-BOC-氨基乙氧基)乙氧基]乙醇

Target: Others, PROTAC Linker

Cat.No: T18617

Synonym: N-(5-氨基戊基)氨基甲酸叔丁酯,PROTAC Linker 23

Target: Others, PROTAC Linker

PROTAC SGK3 degrader-1

Cat.No: T13847

Synonym: SGK3-PROTAC1

Target: SGK

PROTAC RIPK degrader-6

Cat.No: T36243

PROTAC BET Degrader-10

Cat.No: T39374

PROTAC BRD9-binding moiety 1 hydrochloride

Cat.No: T13915L

Synonym: PROTAC BRD9-binding moiety 1 hydrochloride (2097512-23-5 free base)

Target: Others

Soluble Epoxide Hydrolase PROTAC 1a

Cat.No: T83857

Synonym: sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a

Halo PROTAC 1

Cat.No: T17995

Target: Others

PROTAC(H-PGDS)-7

Cat.No: T41267

PROTAC PARP1 degrader

Cat.No: T13845

Target: Others

TBK1 control PROTAC® 4

Cat.No: T36247

PROTAC CDK9 Degrader-1

Cat.No: T5438

Target: CDK

FKBP12 PROTAC RC32

Cat.No: T13694

Synonym: RC32

Target: Others

PROTAC MDM2 Degrader-4

Cat.No: T18634

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T9784	Docosanedioic acid	PROTAC Linker	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。

天然产物

Docosanedioic acid

Cat.No: T9784

Target: PROTAC Linker

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