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Pathways Recommended:	PROTAC

Results for "

Covalent PROTACs

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PROTACs (12) Akt (2) Apoptosis (1) Autophagy (1) E1/E2/E3 Enzyme (1) EGFR (2) Epigenetic Reader Domain (3) ERK (1) Ferroptosis (1) FKBP (1) Glutathione Peroxidase (1) IKK (1) Ligands for Target Protein for PROTAC (1) Mixed Lineage Kinase (1) NF-κB (1) PERK (1) Phosphatase (1) PI3K (1) PROTAC Linkers (4) PROTAC-Linker Conjugates for PAC (1) Ras (1) RIP kinase (1) STING (2)
By Research Areas:	Cancer (16) Infection (1) Inflammation/Immunology (3)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: PROTACs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137516

LC-2 2 Publications Verification	PROTACs Ras	Cancer
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC₅₀s 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 .

HY-129610

KB02-SLF	PROTACs FKBP	Cancer
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 .

HY-129917

KB02-JQ1 4 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
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 .

HY-177119

*ZBP1 Covalent* PROTAC-1**	PROTACs RIP kinase Mixed Lineage Kinase	Infection Inflammation/Immunology
ZBP1 Covalent PROTAC-1 is a covalent Z-DNA binding protein 1 ZBP1 PROTAC degrader, with its DC₅₀ being 25.69 nM. ZBP1 Covalent PROTAC-1 integrates the ligand that recruits the VHL E3 ubiquitin ligase and the DNA aptamer (Aptamer Z3) with the specific Zα domain that can bind to ZBP1, which has a high affinity (K_D = 2.71 nM) with ZBP1. After degrading ZBP1, the phosphorylation levels of downstream signaling molecules RIPK3 and MLKL significantly decrease. ZBP1 Covalent PROTAC-1, encapsulated by nano-liposomes, significantly improves the survival rate of mice infected with influenza A virus (IAV) after administration via the trachea .

HY-156395

MN551 1 Publications Verification	E1/E2/E3 Enzyme	Cancer
MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .

HY-176239

PROTAC PI3Kδ degrader-1	PROTACs PI3K Akt Apoptosis Autophagy	Cancer
PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ *PROTAC* degrader with a DC₅₀ of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC₅₀: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)

HY-144323

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

HY-164977

JCS-1	PROTACs Phosphatase	Cancer
JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3 ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC₅₀ in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .

HY-155075

NC-R17	PROTACs Glutathione Peroxidase Ferroptosis	Cancer
NC-R17 is a PROTAC-class, non-covalent GPX4 degrader based on RSL3, involved in ferroptosis. NC-R17 has antitumor activity and is used for non-covalent GPX4 PROTAC design . NC-R17 consists of a target protein ligand (red part) Demethyl-RSL3 (HY-135832); an E3 ubiquitin ligase ligand (blue part) Lenalidomide (HY-A0003) and a PROTAC linker (black part) (HY-169376). E3 ubiquitin ligase and linker can form Lenalidomide-C13-piperazine-Boc (HY-169377) .

HY-176183

STING ligand-4	Ligands for Target Protein for PROTAC STING	Inflammation/Immunology
STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC₅₀ < 0.2 μM. STING ligand-4 can be used for synthesis of PROTAC STING degrader-4 (HY-176180) .

HY-175240

PROTAC BRD4 Degrader-38	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-38 is a BRD4 *PROTAC* degrader with DC₅₀s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28 .Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)

HY-150905

EGFR ligand-2	EGFR	Cancer
EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC₅₀s of 21 nM and 48 nM for EGFR ^L858R and EGFR ^L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .

HY-176180

PROTAC STING degrader-4	PROTACs STING NF-κB IKK	Inflammation/Immunology
PROTAC STING degrader-4 is a nitro-free covalent STING *PROTAC* degrader with a DC₅₀ of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model . Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181

HY-174415

ZSH-2117	PROTACs EGFR Akt ERK	Cancer
ZSH-2117 is a covalent and selective EGFR *PROTAC* degrader with a DC₅₀ of 45 nM in Ba/F3-EGFR ^{L858R/T790M/C797S} cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR ^{L858R/T790M/C797S} xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker

HY-156388

SCO-PEG8-COOH	PROTAC Linkers	Cancer
SCO-PEG8-COOH is a PROTAC linker and belongs to the PEG class. SCO-PEG8-COOH contains SCO and COOH that can be covalently combined with amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

HY-156387

SCO-PEG4-COOH	PROTAC Linkers	Cancer
SCO-PEG4-COOH is a PROTAC linker and belongs to the PEG class. SCO-PEG4-COOH contains SCO and COOH that can be covalently combined with amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

HY-156386

SCO-PEG3-COOH	PROTAC Linkers	Cancer
SCO-PEG3-COOH is a PROTAC linker and belongs to the PEG class. SCO-PEG3-COOH contains SCO and COOH that can be covalently combined with amino groups respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

HY-156385

SCO-PEG8-NHS	PROTAC Linkers	Cancer
SCO-PEG8-NHS SCO is a PROTAC linker and belongs to the PEG class. SCO-PEG8-NHS SCO contains SCO and NHS esters that can be covalently bound to amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

HY-183939

L1-CIDE-BRM1-13	PROTAC-Linker Conjugates for PAC	Others
L1-CIDE-BRM1-13 (Compound 15) is a linker-drug precursor moiety formed by the covalent conjugation of a PROTAC degrader with a linker for degrader-antibody conjugates (DACs). L1-CIDE-BRM1-13 can be used for the synthesis of DACs .

HY-183575

JQ1-JX5	PROTACs Epigenetic Reader Domain	Cancer
JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC₅₀ of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia .

Cat. No.	Product Name

HY-L945

Sulfonyl Fluoride Fragment Library	1162 compounds
Sulfonyl fluoride (-SO₂F) overcomes the bottleneck of target selectivity in traditional covalent warheads through its unique chemical and biological properties, which rely heavily on cysteine (Cys) residues. Featuring high stability and tunable electrophilicity under physiological conditions, it can target a wide range of nucleophilic residues including lysine (Lys), tyrosine (Tyr), serine (Ser), and histidine (His). It offers the advantages of a broader druggable space, lower off-target risks, and long-lasting efficacy, with numerous reported cases in the research of covalent inhibitors, Molecular glue, PROTACs, and chemical biology probe development. MCE constructs a highly diverse sulfonyl fluoride fragment library based on the reactivity, stability and physiological compatibility of sulfonyl fluoride. The library contains 1000 efficiently synthesized and stable sulfonyl fluoride fragments, which ensure precise reactivity of the warhead and retain sufficient derivatization space for subsequent optimization. Combined with the modular strategy of SuFEx click chemistry, it enables versatile modification of compounds and functionalization of complex molecules, improves the efficiency of structural optimization and rapidly expands druggability, making it suitable for high-throughput probe and custom covalent library construction. It provides an efficient research tool for the development of broad-spectrum covalent inhibitors targeting Lys/Tyr/Ser/His, covalent PROTACs for E3 ligases and chemical biology probe development, meeting the requirements of modern drug research for high throughput, high success rate and high derivatization potential. This library contains 1,162 sulfonyl fluoride fragments with high structural diversity, favorable drug-like properties and tunable electrophilicity. It is well suited for precise targeting of non-Cys residues and meets the criteria of simple structure and high derivatization potential. It effectively improves

Sulfonyl Fluoride Fragment Library

1162 compounds

Sulfonyl fluoride (-SO₂F) overcomes the bottleneck of target selectivity in traditional covalent warheads through its unique chemical and biological properties, which rely heavily on cysteine (Cys) residues. Featuring high stability and tunable electrophilicity under physiological conditions, it can target a wide range of nucleophilic residues including lysine (Lys), tyrosine (Tyr), serine (Ser), and histidine (His). It offers the advantages of a broader druggable space, lower off-target risks, and long-lasting efficacy, with numerous reported cases in the research of covalent inhibitors, Molecular glue, PROTACs, and chemical biology probe development.

MCE constructs a highly diverse sulfonyl fluoride fragment library based on the reactivity, stability and physiological compatibility of sulfonyl fluoride. The library contains 1000 efficiently synthesized and stable sulfonyl fluoride fragments, which ensure precise reactivity of the warhead and retain sufficient derivatization space for subsequent optimization. Combined with the modular strategy of SuFEx click chemistry, it enables versatile modification of compounds and functionalization of complex molecules, improves the efficiency of structural optimization and rapidly expands druggability, making it suitable for high-throughput probe and custom covalent library construction. It provides an efficient research tool for the development of broad-spectrum covalent inhibitors targeting Lys/Tyr/Ser/His, covalent PROTACs for E3 ligases and chemical biology probe development, meeting the requirements of modern drug research for high throughput, high success rate and high derivatization potential.

This library contains 1,162 sulfonyl fluoride fragments with high structural diversity, favorable drug-like properties and tunable electrophilicity. It is well suited for precise targeting of non-Cys residues and meets the criteria of simple structure and high derivatization potential. It effectively improves

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