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
T13786	MZP-55	MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)
T13657	dMCL1-2	dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, which binds to MCL1 with a KD of 30 nM. dmcl-2 activates the apoptosis mechanism by degrading MCL1.This compound is unstable in powder form and other related salt forms are recommended.
T12552	PROTAC CDK2/9 Degrader-1	PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).
T18604	PROTAC CRBN Degrader-1	PROTAC CRBN Degrader-1 is a chemical compound consisting of a cereblon (CRBN) ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group. It functions as a cereblon (CRBN) degrader[1].
T13887	SJF620	SJF620 is a potent degrader of PROTAC BTK(DC50 : 7.9 nM).
T13782	MS432	MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
T17543	BI-3663	BI-3663 is a highly selective PTK2/FAK PROTAC that utilizes cereblon ligands to hijack E3 ligases for PTK2 degradation, with an IC50 of 18 nM. It is composed of BI-4464 linked to Pomalidomide with a linker[1]. Anti-cancer.
T13105	TD-428	TD-428 is a highly specific degrader of BRD4(DC50 of 0.32 nM). TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
T17926	(S,R,S)-AHPC-PEG6-C4-Cl	(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
T13840	PROTAC FAK degrader 1	PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.
T13930	TL13-12	TL13-12 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.69 nM).
T13833	PROTAC BRD4 Degrader-1	PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).
T13743	JH-XI-10-02	JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.
T13845	PROTAC PARP1 degrader	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).
T12907	SIAIS178	SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
T14318	ARCC-4	ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].
T10485	PROTAC Bcl2 degrader-1	PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).
T12027	MG-277	MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.
T13844	PROTAC K-Ras Degrader-1	PROTAC K-Ras Degrader-1 is potent degrader of K-Ras based PROTAC.
T18597	dFKBP-1	dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].

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PROTAC Selection