protac linker-10

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。

Tetraethylene glycol是一种PEG类的PROTAC Linker,可以作为Polyethylene glycol dehydrogenase的底物而被氧化(Km=10mM)。

Br-C10-methyl ester 是一种属于 alkyl ether 类的 PROTAC linker，可用于一系列 PROTAC 分子的合成。PROTAC 分子含有两个通过 linker 连接的不同配体，一种是 VHL 配体部分，另一种是靶蛋白配体。

Azido-PEG10-alcohol 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。

Amino-PEG10-acid 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。

Fmoc-NH-PEG10-acid 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。

Hydroxy-PEG10-acid (HO-PEG10-CH2CH2COOH) 是 PEG 类 PROTAC linker。可用于合成 PROTAC 分子。

(10-BRomodecyl)phosphonic acid is an alkyl chain-derived PROTAC linker suitable for PROTAC synthesis [1].

The compound [10-(diethoxy-phosphoryl)-decyl]-phosphonic acid is a suitable alkyl chain-based PROTAC linker for the synthesis of PROTACs [1].

Diethyl 10-bromodecylphosphonate is an alkyl-based PROTAC linker utilized for the synthesis of PROTACs[1].

m-PEG10-alcohol, also known as Decaethylene glycol monomethyl ether, is a non-cleavable 10 unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1]. Additionally, m-PEG10-alcohol serves as a PEG-based PROTAC linker, enabling its application in the synthesis of PROTACs[1].

Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1].

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker，是一种合成的 E3 连接酶配体-linker 偶联物 (E3 ligase ligand-linker conjugate)。用于 BET 的靶向 PROTAC 的合成。

cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10.

Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1].

Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].

Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1].

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker，是一种合成的 E3 连接酶配体-linker 偶联物，用于合成 BET 的靶向 PROTAC。

SJFδ is a 10-atom linker PROTAC that selectively degrades p38δ with a DC50 of 46.17 nM, without degrading p38α, p38β, or p38γ[1].

E3 Ligase Ligand-linker Conjugate 134，作为E3 连接酶配体与接头的复合体（conjugate of E3 ligase Ligand and linker），是制造PROTAC活性分子STING-IN-10的核心中间体。

Acepromazine-1-Piperazinepropanamine (compound 10) 为一种 E3 连接酶配体-linker 偶联物 (E3 Ligase Ligand-Linker Conjugate)，结合了cereblon配体及其 linker。该化合物通过靶蛋白配体连接技术，能够生成 PROTAC分子，命名为 TrimTAC1。

PROTAC BTK Degrader-10 (Example 1P) 是一种靶向BTK的PROTAC降解剂，用于慢性淋巴细胞白血病 (CLL) 的研究。(Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)

PROTAC JNK1-targeted-1 (PA2) 是一种 JNK1 PROTAC 降解剂，具有 DC50 值为 10 nM。此化合物能够降低纤连蛋白水平，并可用于肺纤维化研究。(Pink: JNK1 inhibitor; Black: linker; Blue: CRBN Ligand)

ND1-YL2 is a peptide-based PROTAC®Degrader of steroid receptor co-activator 1 (SRC-1; also known as nuclear receptor coactivator 1, NCOA1). ND1-YL2 is composed of a stapled peptide that binds SRC-1 (YL2) joined by a linker to a tetrapeptide that binds UBR box domains. Upon ternary complex formation, SRC-1 is polyubiquitinated and subsequently degraded via the N-degron pathway. This Degrader induces dose-dependent degradation of SRC-1 in the MDA-MB-231 triple negative breast cancer cell line (DC50 = 10 μM), and binds to the PAS-B domain of SRC-1 (Ki = 320 nM). ND1-YL2 inhibits MDA-MB-231 cell migrationin vitro, and suppresses metastasis of MDA-MB-231 cellsin vivo.