PROTAC Selection

产品编号	产品名称
T13834	PROTAC BRD4 Degrader-2	PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).
T11975	PROTAC Mcl1 degrader-1	PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
T18636	PROTAC ERα Degrader-1	PROTAC ERα Degrader-1 is a chemical compound. It consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group. This compound serves as a degrader of estrogen receptor-alpha (ERα).
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.
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].
T18680	SD-36	SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse models.
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, with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes 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) (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].

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PROTAC Selection