dc50

ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade

SJFα (SJF alpha) is a PROTAC formed by an E3 ubiquitin ligase-conjugated protein hydrolysis regulator that degrades p38α and p38δ and can be used in cancer research.

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].

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to an LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM for ABL, 10 nM for cIAP1, 12 nM for cIAP2, and 50 nM for XIAP[1].

TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1].

ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

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).

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

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.

CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.

iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1. iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach.

MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

MT-802 is an effective BTK degrader based on PROTAC technology (DC50: 1 nM). MT-802 has the potential to treat C481S mutant chronic lymphocytic leukemia (CLL).

VZ185 is an effective and selective dual BRD7/9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively).

ZXH-3-26 is a PROTAC composed of a Cereblon ligand, an E3 ubiquitin ligase, and a BRD4 ligand that can be used to study cancer.

PROTACKSP-IN-1 (Compound 21) is a spindle protein (KSP) degrader as a PROTAC, effectively degrading KSP in HCT-116 cells with a DC50 value of 114.8 nM. It inhibits the proliferation of HCT-116 with an IC50 of 10 nM, causes G2/M phase cell cycle arrest, and induces apoptosis in HCT-116. Additionally, PROTACKSP-IN-1 demonstrates antitumor activity in mouse models.

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader specifically targeting PARP1, with a DC50 of 58.14 nM. It demonstrates cytotoxicity in SW-620 and LOVO cancer cells, with IC50 values of 1.63 μM and 2.84 μM, respectively. In BRCA-mutated colon cancer cells, PROTAC PARP1 degrader-3 exhibits synergistic effects with SN-38, with a combination index (CI) of 0.487.

AB3067 is a PROTAC degrader targeting BET protein, efficiently recruiting two distinct E3 ligases, Cereblon and VHL, with strong affinity (demonstrated by IC50 values of 559 nM for VHL and 190 nM for CRBN in vivo HEK293). It degrades BRD2, BRD3, BRD4, and CRBN with DC50 values of 2.1~2.3, 1.6, 15, and 75 nM, respectively. Additionally, AB3067 inhibits the proliferation of RKO cells, with an EC50 of 111 nM. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL and CRBN)

PROTAC JNK1-targeted-1 (PA2) is a JNK1 PROTAC degrader with a DC50 of 10 nM. It effectively reduces fibronectin levels and is useful in lung fibrosis research. [Pink: JNK1 inhibitor; Black: linker; Blue: CRBN Ligand]

PROTAC BRD4 Degrader-29 (compound 7a) is a potent BRD4 PROTAC degrader with a DC50 of 89.4 nM, playing a significant role in cancer research.