PROTAC Bcl-xL ligand-1 is a ligand for Bcl-xL that can be used in the synthesis of PROTACs.

BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1.

Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.

Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128.

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.

ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

Mal-PEG2-NH2 (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.

BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.

PROTAC ER Degrader-2 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).

SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM.

SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.

SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM.

SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-1 induces cancer cell death.

SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-2 induces cancer cell death.

PROTAC PTK6 ligand-1 is an intermediate for BTK kinase inhibitor preparation. PROTAC PTK6 ligand-1 can be used in the synthesis of ARD-61.

OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.

Boc-bipiperidine-ethynylbenzoic acid is an Alkyl/ether-based PROTAC linker can be used in the synthesis of ARD-61.

L-Homopropargylglycine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine hydrochloride is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor.

Dovitinib RIBOTAC is a targeted RNA degrader that cleaves pre-miR-21 with enhanced potency and selectivity.

Propargyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotinyl-NH-PEG3-C3-amido-C3-COOH (DIPEA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

1-Bromo-6-chlorohexane is a PROTAC linker can be used in the synthesis of PROTACs.

Bromo-C10-OBn is a PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.

PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

TLR4-IN-C34-C2-amide-C6-OH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

Biotin-PEG8-Vidarabine is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

Biotin-PEG7-C2-S-Vidarabine is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

Biotin-PEG7-C2-NH-Vidarabine-S-CH3 is a PEG-based linker that incorporates adenosine analog Vidarabine. Vidarabine is an antiviral agent which is active against herpes simplex and varicella zoster viruses.

ATP-PEG8-Biotin is a PEG-based linker that incorporates ATP. ATP is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary affinity to VHL (Kd=125 nM). AGB1 exhibits favorable pharmacokinetic profile in mice with the DC50, 6 h of ∼13 nM.

Boc-NH-PEG11-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Di(N-succinimidyl) adipate (DSAP) is an alkyl chain-based PROTAC linker that is applicable to the synthesis of PROTACs.

tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker that refers to the PEG composition. tert-Butyl 11-aminoundecanoate is applicable to the synthesis of a series of PROTACs.

TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.

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

L-Azidohomoalanine-1,2,3,4-13C4 hydrochloride is the 13C- and 15N-labeled L-Azidohomoalanine hydrochloride. L-Azidohomoalanine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

2-(2-(6-chlorohexyloxy)ethoxy)ethanamine (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

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

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

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

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

Amino-PEG6-acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-N-amido-PEG2-C6-Cl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-Aminooxy-PEG4-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Bromo-PEG5-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

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

Bromo-C4-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

BocNH-PEG5-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Br-PEG6-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Triethylene glycol monododecyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Cbz-PEG5-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Bromo-PEG7-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-Aminooxy-PEG4-t-butyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

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

Boc-NH-PEG7-acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Acid-PEG7-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Bromo-PEG8-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

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

Bis-PEG4-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

N-Boc-PEG10-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Amino-PEG11-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Acid-PEG9-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

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

t-Boc-amido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-N-amido-PEG10-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Acid-PEG10-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG6-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-Aminooxy-PEG11-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG9-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG10-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Acid-PEG12-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

m-PEG15-acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

N-bis(t-boc-N-amido-PEG3)-N-(PEG3-acid) hydrochloride is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Acid-PEG14-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HO-PEG18-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG10-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

t-Boc-N-amido-PEG15-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

m-PEG18-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

ML 2-14 is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. ML 2-14 can be used in the synthesis of the PROTAC.

Mal-amido-PEG15-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-Thalidomide is a cereblon affinity probe for PROTAC and targeted protein degradation research.

C18-PEG13-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DBCO-N-bis(PEG4-NHS ester) is a PEG linker which contains two PEG4-NHS ester and a DBCO group. DBCO-N-bis(PEG4-NHS ester) is useful for protein modification or labeling.

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

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

DBCO-PEG6-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

TCO-PEG2-Sulfo-NHS ester sodium is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).

MS 177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in mice.

MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs.

PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells.

TSPO ligand-1 is the ligand of AUTAC4 that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.

dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.

4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs.

cis-MZ 1 is a negative control of MZ 1. cis-MZ 1 is a PROTAC targeting to BRD4.

MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity.

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].

TCIP1 is the most potent transcriptional/epigenetic CIP (chemical inducers of proximity) and specifically activates BCL6 target genes. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines and exhibits cell-specific and tissue-specific effects. TCIP1 successfully killed large B cell lymphoma cell lines, including chemotherapy-resistant TP53-mutant lines and exhibited cell-specific and tissue-specific effects. The activation of apoptosis to cell death took place in just 72 hours.BCL6 is critical to the lymphatic system, and mice engineered without the BCL6 gene die of complex inflammatory reactions. BRD4 is heavily involved in genome function and stability across many processes. Concerns regarding utilizing these important gene expressions and how they might affect off-target healthy tissues were addressed in the study.TCIP1 acts in a context-specific manner requiring the expression of BRD4 and BCL6 to both be present in order to bind them and operate at a concentration that would occupy only a tiny fraction of the total BCL6 molecules.TCIP1 induced dramatic transcriptomic changes in the spleen, notably with an upregulation of the FOXO3 gene, which mirrored activity in the targeted cancer cells. Despite the significant transcriptomic changes in the spleen, TCIP1 was well tolerated without adverse effects, with no significant differences in mouse body weight and no noticeable abnormalities such as inflammatory infiltrates or apoptotic cells. BCL6-BRD4 TCIP1 (TCIP1) is a potent BCL6-BRD4 transcriptional/epigenetic chemical inducer of proximity (TCIP) by covalently linking BCL6 binder BI-3812 to BRD4 ligand JQ1, selectively kills DLBCL cells with EC50 of 1.3 nM against KARPAS422 cell. TCIP1 rapidly and robustly killed other DLBCL lines with high levels of BCL6, but JQ1 and BI3812 separately or together shows100–1,000-fold less-effective cell killing. TCIP1 is 200–10,000-fold more potent in killing DLBCL cells than the degradation of BRD4 by dBET1 and/or degradation of BCL6 by BI3802. TCIP1 induces a stable, cooperative protein-protein interaction between bromodomain 1 (BD1) of BRD4 and the BTB domain of BCL6. TCIP1 shows affinity for intracellular ternary complex of BRD4 with Kd of 340 nM in TR-FRET assays. TCIP1 induces G1/S and G2/M block in the cell cycle, TCIP1 (10 nM) represses MYC and its targets while activating pro-apoptotic genes in KARPAS422 cells. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines, at EC50 of 1-10 nM in 72 h and exhibits cell-specific and tissue-specific effects, capturing the combinatorial specificity inherent to transcription.

ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer.

Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design.

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.

ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.

BI 1810284 (ACBI2, BI 01810284) is a potent, selective and orally bioavailable VHL-recruiting PROTAC degrader of SMARCA2 (DC50=1 nM in RKO cells), 30-fold selectivity over SMARCA4.

BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon.

BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

BTX-6654 is a potent, selective SOS1 cereblon-based bifunctional PROTAC degrader, reduces downstream signaling markers, pERK and pS6, and displayed antiproliferative activity in cells harboring various KRAS mutations.

BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.

CC-3240 is a molecular glue degrader of CaMKK2 based on CC-8977 with bingding IC50 of 9 nM and DC50 of 100 nM (THP1 cells, Dmax=92%).

Chk1 PROTAC-2 is a potent Chk1 degrader with DC50 of 1.33 µM in A375 cells.

CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells.

CRBN(FLT3)-8 a highly potent FLT3 degrader by introducing gilteritinib into targeted protein degradation technology, potently degrades FLT3-ITD via UPS and inhibits the proliferation of FLT3-ITD mutant AML cells more effectively than gilteritinib.

DAS-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 3 nM, without effect on Bcr-Abl.

DAS-CHO-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 62 nM in CAL148 cells.

DB0614 is a CRBN-based PROTAC, induces the degradation of NEK9, FAK, CDK4, CDK6, and WEE1 in cells.

DBt-10 is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays.

dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib.

DeFer-2 is an oleic acid (OA)-based ferritin-targeting PROTAC binding Kd of 17.1 uM, degrades ferritin and rapidly elevates the free iron content, induces pyroptosis.

Degradomer D-1 is a selective proteasomal degrader of IRAK3 with Kd of 100 nM, DC50 of 94 nM, displays no binding affinity against IRAK4 (Ki >10 uM).

DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment.

GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).

HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.

HPP-9 is a potent BET bromodomain degrader that acts through a PROTAC mechanism, HPP-9 is a long-acting Hedgehog pathway inhibitor.

INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).

JCS-1 is a RG3039-based degarder (PROTAC) of the RNA decapping scavenger protein DcpS exhibiting effective degradation of DcpS at nanomolar concentrations, non-covalently binds DcpS and recruits the E3 ligase VHL, induces potent, rapid, and sustained DcpS

JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line.

JH-XII-03-02 is a highly potent, selective PROTAC degrader of LRRK2 with IC50 of 1 nM against both wt LRRK2 and LRRK2 G2019S.

JWZ-1-80 is a potent and selective PROTAC degrader of PI5P4Kγ with Kd of 510 nM, 1 uM induces 75% reduction of PI5P4Kγ in Molt4 cells.

KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PTORAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggerin

KYH1872 is a PROTAC that induces protein degradation via the KLHDC2 E3 ubiquitin ligase, KYH1872 is consisted of a C-terminal fragment of the SelK protein and promiscuous kinase inhibitor YHJ1039 via PGE linker.

LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins.

MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.

MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitinatio

MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.

MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively.

PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.

PROTAC dCE-1 is a potent, selective CBP/EP300 degrader targeting the histone acetyltransferase (HAT) domain, with DC50 value of 1.3 μM in LP1 cells.

PTD10 is a highly potent BTK PROTAC degrader with DC50 of 0.5 nM in TMD8 cells, inhibits cell growth and induces apoptosis more potently than parent molecule GDC-0853.

QA-68-ZU81 (QA-68) is a EA-89-based BRD9 degrader that incorporates the EA-89 warhead into a cereblon (CRBN)-targeting proteolysis-targeting chimera (PROTAC).

SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%.

TD-802 is potent, cereblon-mediated androgen receptor PROTAC degrader, effectively inducs AR protein degradation with DC50 of 12.5 nM and Emax 93% in LNCaP prostate cancer cells.

TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.

TMX-4153 (TMX4153) is a bivalent PIP4K2C degrader (MOLT4 cells, DC50=24 nM, Dmax=921% at 1 uM) based on TMX-4084, rapidly and selectively degrades endogenous PIP4K2C.

U7D-1 is a selective USP7-degrading Proteolysis Targeting Chimera (PROTAC). U7D-1 showed selective and effective USP7 degradation, and maintained potent cell growth inhibition in p53 mutant cancer cells.

UBX-382 (UBX382) is a potent and orally available proteolysis-targeting chimera (PROTAC) that induces potent BTK degradation in DLBCL cell line with DC50 of 4.5 nM.

UNC7700 (UNC-7700) is a potent EED-targeted PRC2 degrader, contains a unique cis-cyclobutane linker and potently degrades all PRC2 components EED (DC50=111 nM; Dmax=84%), EZH2WT/EZH2Y641N (DC50=275 nM; Dmax=86%) and SUZ12 (Dmax=44%) in DLBCL cells.

WD6305 is a potent and selective proteolysis-targeting chimera (PROTAC) degrader of METTL3-METTL14 complex with DC50 of 140 nM (METTL3), Dmax of 91.9% in Mono-Mac-6 AML cell line.

MS40 is a cereblon (CRBN)-based proteolysis targeting chimera (PROTAC) degrader of the onco-target WD repeat domain 5 (WDR5) [1]. WDR5 is an integral component of the MLL/KMT2A lysine methyltransferase protein complex. The WDR5-binding component of MS40 is the selective inhibitor OICR-9429, and the CRBN-targeting moiety is the immunomodulatory drug pomalidomide. MS40 promotes degradation of WDR5 and the pomalidomide transcription factor neo-substrates IKZF1 and IKZF3.

XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.

YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).

ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%).