PROTAC Selection

Selection of target proteins for PROTAC can be based on the following considerations: 1. Whether the protein is specific or not, non-specific proteins can cause off-target toxicity; 2. Whether the protein belongs to the molecules that can be degraded by PROTAC, and it has been reported that the targets that can be used for PROTAC include, kinases (MEK, KRAS, CDK, and Bcr/Abl), transcription factors (e.g. p53, STAT, RAR, ER, and AR), epigenetic factors (e.g., HDAC and BET bromodomain), and E3 ligases themselves (e.g., MDM2), among others; 3. Whether or not the protein has been reported to have a ligand or crystalline form that can be commercially engineered.

产品编号	产品名称
T16667	PROTAC Sirt2 Degrader-1	PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].
T17249	VZ185	VZ185 is an effective and selective dual BRD7/9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively).
T11292	FKBP12 PROTAC dTAG-7	FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
T13839	PROTAC ER Degrader-4	PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.
T11664	INY-03-041	INY-03-041, a potent and highly selective PROTAC-based pan-AKT degrader, inhibits AKT1, AKT2, and AKT3 with IC50s of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. This compound consists of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide.
T12556	PROTAC B-Raf degrader 1	PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.
T84316	ARV-393	ARV-393 是一种 BCL6 PROTAC 降解剂，在 DLBCL 和 BL 细胞系中的 DC50 和 GI50 值均 <1 nM。ARV-393 在多个肿瘤异种移植模型中，可起到抑制肿瘤体积的作用。
T13846	PROTAC RIPK degrader-2	PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
T13849	PROTAC BET Degrader-1	PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.
T18631	PROTAC MDM2 Degrader-1	PROTAC MDM2 Degrader-1 is a chemical compound that utilizes PROTAC technology to degrade MDM2. This compound is comprised of a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].
T18633	PROTAC MDM2 Degrader-3	PROTAC MDM2 Degrader-3 is a compound that leverages PROTAC technology to degrade MDM2. It consists of a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].
T18607	PROTAC ER Degrader-3	PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].
T17910	(S,R,S)-AHPC-PEG2-C4-Cl	(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
T17911	(S,R,S)-AHPC-C6-PEG3-C4-Cl	(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
T13842	PROTAC IRAK4 degrader-1	PROTAC IRAK4 degrader-1 is a PROTAC (proteolysis-targeting chimera) compound that targets and degrades interleukin-1 receptor-associated kinase 4 (IRAK4).
T13835	PROTAC BRD4 Degrader-3	PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.
T13785	MZP-54	MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)
T14549	BETd-246	BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
T12560	PROTAC BRD9 Degrader-1	PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.
T16701	QCA570	QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).

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PROTAC Selection