PROTAC Degrader

Cat. No.

A18712

CAS No.

2136247-12-4

MD-224

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.

Cat. No.

A12563

CAS No.

2093388-62-4

BETd-260

Synonyms: ZBC 260

BETd-260 is a potent BET degrader based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.

Cat. No.

A13255

CAS No.

1949837-12-0

ARV-771

ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

Cat. No.

A16858

CAS No.

1799711-21-9

dBET1

dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.

Cat. No.

A18355

CAS No.

2378801-85-3

PROTAC Bcl2 degrader-1

PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.

Cat. No.

A18378

CAS No.

2351218-88-5

dMCL1-2

dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.

Cat. No.

A18399

CAS No.

2243076-67-5

ZXH-3-26

ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM.

Cat. No.

A18446

CAS No.

2320561-35-9

ERD-308

ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.

Cat. No.

A18519

CAS No.

2158322-29-1

PROTAC ER Degrader-3

PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

Cat. No.

A18589

CAS No.

2231744-29-7

MT-802

MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).

Cat. No.

A18682

CAS No.

2230826-81-8

PROTAC FLT-3 degrader 1

PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.

Cat. No.

A18685

CAS No.

2306193-61-1

VZ185

VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively.

Cat. No.

A18735

CAS No.

2064292-12-0

A1874

A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.

Cat. No.

A18785

CAS No.

2093388-33-9

PROTAC BET degrader-2

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.

Cat. No.

A18863

CAS No.

2358775-70-7

PROTAC CRBN Degrader-1

PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.

Cat. No.

A18904

CAS No.

2306388-85-0

PROTAC ERRα Degrader-2

PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.

Cat. No.

A18910

CAS No.

2306388-84-9

PROTAC ERRα Degrader-1

PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.

Cat. No.

A19081

CAS No.

2064175-32-0

FKBP12 PROTAC dTAG-7

Synonyms: dTAG-7

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader.

Cat. No.

A19088

CAS No.

2139287-33-3

THAL-SNS-032

THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

Cat. No.

A19133

CAS No.

1883863-52-2

dBET57

dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology.

Cat. No.

A19334

CAS No.

2244520-98-5

Homo-PROTAC cereblon degrader 1

Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

Cat. No.

A19342

CAS No.

2244684-49-7

Homo-PROTAC pVHL30 degrader 1

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC.

Cat. No.

A19415

CAS No.

2010159-48-3

MZP-55

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.

Cat. No.

A19426

CAS No.

2010159-47-2

MZP-54

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

Cat. No.

A19437

CAS No.

2098836-50-9

AT6

AT6 is a PROTAC AT1 analogue, which is a highly selective bromodomain (Brd4) degrader.