A heterobifunctional small molecule PROTAC capable of cereblon mediated proteasomal degradation of CDK9.

CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.

A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε.

A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM)..

A PEG linker for PROTAC..

A PEG linker for PROTAC..

A PEG linker for PROTAC..

A PEG2 linker for PROTAC..

A PEG3 linker for PROTAC..

A PEG4 linker for PROTAC..

A VHL ligand for PROTAC..

A VHL ligand for PROTAC..

A VHL ligand for PROTAC..

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).

Alprostadil(Caverject) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

An E3 ligand- Linker Conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC.

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC..

An E3 ligase ligand-linker conjugate for PROTAC.

An E3 ligase ligand-linker conjugate for PROTAC...

ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.

BTK PROTAC 10 is a novel potent PROTAC for BTK with DC50 of 1.1 nM in cultured Ramos cells.

BTK PROTAC 9 is a novel potent PROTAC for BTK with DC50 of 5.9 nM in cultured Ramos cells, requires simultaneous engagement of BTK and CRBN to effectively degrade BTK.

CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1.

CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein[1].

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

dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.

dBRD9 is a PROTAC that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex.

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).

E3 Ligand-Linker Conjugate 5 is an E3 ligase ligand-linker conjugate for PROTAC..

E3 ligase Ligand 1 dihydrochloride is a Hippel-Landau (VHL) E3 ligase-binding moiety based on PROTAC technology.

E3 ligase Ligand 1A is a ligand of E3 ligase, used in PROTAC technology; E3 ligase Ligand 1A can be used in the research of cancer. (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL)

E3 ligase Ligand 2 is a Ligand for E3 Ligase used in PROTAC technology.

E3 ligase Ligand 3 is a ligand of E3 ligase, used in PROTAC technology.

E3 Ligase Ligand-Linker Conjugates 22 incorporates an E3 ligase ligand and a linker, can be used for the treatment of EZH2-mediated cancer.

E3 Ligase Ligand-Linker Conjugates 23 (TFA) is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

E3 Ligase Ligand-Linker Conjugates 25 Trifluoroacetate is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

HDAC6 degrader 9c (dHDAC6 9c) is a bifunctional molecule (dHDAC6) that could selectively degrade HDAC6, by conjugating non-selective HDAC inhibitor to a thalidomide-type E3 ligase ligand.

MDK7526, also known as VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader.

MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).

MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.

PROTAC-VHL-ligand is a von Hippel–Lindau (VHL) ligand used for the proteolysis targeting chimeras (PROTACs) method, induces target protein degradation..

QCA570 is a novel, highly potent efficacious BET degrader (PROTAC).

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.

SNIPER(ABL)-062 is a novel, potent SNIPER molecule that tethers BCR-ABL inhibitor to a ligand of IAP, causes potent BCR-ABL degradation.

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

VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM..

VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.

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 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.

CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.

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.

Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

THP-PEG6-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. THP-PEG6-OH is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.

XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1.

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.

NH2-PEG5-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH2-PEG5-OH is also a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker.

KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.

(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to VHL and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).

GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).

PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.

NH2-PEG6-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH2-PEG6-Boc is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Azido-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-alcohol is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.

DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.

PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.

PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.

Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.

CC-90009 is a cereblon modulator. CC-90009 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3), which are transcriptional repressors in T-cells. This reduces the levels of these transcription factors, and modulates the activity of the immune system, which may include the activation of T-lymphocytes. .

ARD-266 is a a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.

PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1.

SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

PROTAC ER Degrader-4 is a PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.

PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC BRD4 degrader.

NH2-PEG2-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH2-PEG2-C2-Boc is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

N3-PEG3-CH2CH2COOH a PEG-based PROTAC linker can be used in the synthesis of BI-3663, BI-4216 and BI-0319. Azido-PEG3-acid is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Amino-PEG4-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Amino-PEG4-alcohol is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Boc-NH-PEG4-CH2CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC. Boc-NH-PEG4-CH2CH2COOH is also a cleavable ADC linker used as a linker for antibody-drug conjugates (ADC).

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein[1].

Vipivotide tetraxetan Ligand-Linker Conjugate (PSMA-617 Ligand-Linker Conjugate) is composed of a linker and Glutamate-urea-Lysine, can be used to synthesize Vipivotide tetraxetan (PSMA-617). Glutamate-urea-Lysine is is the selective pharmacophore to bind to prostate specific membrane antigen (PSMA).

VH 032 Linker 2 is a derivative of the proteolysis-targeting chimera technology (PROTAC) building block VHL ligand 1.

Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs.

PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).

PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).

PROTAC RIPK degrader-6 (example 1) is a PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder.

PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, with a DC50 of 49 nM.

Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader.

VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs.

ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.

Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1. PROTAC B-Raf degrader 1 has anti-cancer activity.

Pomalidomide 4'-alkylC5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.

(S,R,S)-AHPC-Me-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C5-COOH can be used in PROTAC DT2216.

Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the?Thalidomide?based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22)?synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib.

HS-PEG3-CH2CH2NH2 hydrochloride (Thiol-PEG3-amine hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.

Thalidomide-O-C8-Boc is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-Boc can be connected to the ligand for protein by a linker to form PROTACs.

N-Boc-piperazine-C3-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-N-piperazine-C3-COOH can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1.

Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1. PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM.

KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 and KB02-SLF.

(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker.

(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.

Folate-PEG3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG1-mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG3-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HyNic-PEG2-TCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HyNic-PEG2-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Boc-HyNic-PEG1-mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Boc-HyNic-PEG2-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Boc-HyNic-PEG2-N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Boc-HyNic-PEG2-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Mal-amide-PEG2-oxyamineBoc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Methyltetrazine-PEG4-amine (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Bromoacetamide-PEG3-C1-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Mal-amide-PEG2-oxyamine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Methyltetrazine-PEG4-SSPy is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DBCO-C2-SulfoNHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

Bis-BCN-PEG1-diamide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker.

PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines.

Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders.

(S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.

Aldehyde-benzyl-PEG5-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

6-Maleimidocaproic acid sulfo-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

3-Mercaptopropanyl-N-hydroxysuccinimide ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

Mal-amino-sulfo is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.

(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.

BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.

A 410099.1, amine-Boc hydrochloride is a?functionalized IAP ligand for PROTACs. that is incorporates with an amine functional handle for ready conjugation to a linker/target protein ligand.

A 410099.1 amide-PEG3-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG3-amine-Boc can conjugates with target protein ligands.

A 410099.1 amide-PEG2-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG2-amine-Boc can conjugates with target protein ligands.

Boc-A 410099.1 amide-alkylC4-amine is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-alkylC4 linker with terminal amine. Boc-A 410099.1 amide-alkylC4-amine can conjugates with target protein ligands.

Thiol-PEG-Tetrazine (MW 5kDa) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC KRASG12C Degrader-LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. PROTAC KRASG12C Degrader-LC-2 is composed of a covalent KRAS G12C inhibitor MRTX849, a VHL ligand and a linker.

Pomalidomide-PEG1-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology.

N-(Amino-PEG2)-N-bis(PEG3-azide) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

L-Azidohomoalanine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG4-hydrazide (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.

N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1.

Amino-PEG4-C1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

endo-BCN-O-PNB is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

Br-C3-methyl ester is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1.

Maleimide-C10-NHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

m-PEG7-thiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

NH2-PEG1-C1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Thalidomide 5-fluoride is Thalidomide-based cereblon ligand?that incorporates to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

Homo-PROTAC cereblon degrader 1, is a cereblon degrader.

Thalidomide-O-amido-C3-PEG3-C1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Thalidomide-NH-PEG8-Ts is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 8-unit PEG linker used in PROTAC technology, such as IDO1 PROTAC degrader.

CP5V is a PROTAC, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation.

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells.

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

Lenalidomide-I (Compound 72) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570.

Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032.

CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.

Pomalidomide-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.

Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Pomalidomide 4'-PEG5-acid (Pomalidomide-PEG5-CO2H) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 5-unit PEG linker used in PROTAC technology.

(S,R,S)-AHPC-PEG5-Boc is a E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for Cdc20 degrader CP5V.

Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate which can be used for synthesizing dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.

Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.

Thalidomide-NH-PEG4-Ms is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739.

Thalidomide-NH-C2-PEG3-OH is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739.

Tos-O-C4-NH-Boc is an alkyl ether-based PROTAC linker can be used in the synthesis of PROTACs, such as BSJ-03-204

A Novel PROTACs building block.

Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC

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

BOC-NH-PEG2-propene is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Propenyl-PEG3-Propenyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

H2N-PEG2-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Benzyl-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Hydroxy-PEG4-methyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Boc-NH-PEG-Thiol (MW 10000) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

m-PEG750-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

NH2-PEG-Strt (MW 10000) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

NH2-PEG-Strt (MW 3000) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.