covalent ligand

By Targets:	ADC Linker (1) Aldehyde Dehydrogenase (ALDH) (1) AUTACs (1) Autophagy (1) Bcl-2 Family (1) c-Myc (1) Cannabinoid Receptor (1) E1/E2/E3 Enzyme (1) EGFR (2) Epigenetic Reader Domain (1) FKBP (1) Fluorescent Dye (1) PERK (1) PROTACs (3) Ras (1)
By Research Areas:	Cancer (16) Inflammation/Immunology (2) Neurological Disease (1)
Click Chemistry:	DBCO (1) Alkynes (1)

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134761

EN4	c-Myc	Cancer
EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis .

HY-W229874

EN106	Others	Cancer
EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1 .

HY-151716

Halo-DBCO	ADC Linker	Others
Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples.

HY-143346

CCW16

Others Cancer

CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders .

CCW16	Others	Cancer
CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders .

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-122577

EN40

Aldehyde Dehydrogenase (ALDH) Cancer

EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀ value of 2 uM

EN40	Aldehyde Dehydrogenase (ALDH)	Cancer
EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀ value of 2 uM

HY-D2270

Halo tag TMR	Fluorescent Dye	Others
Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and high affinity .

HY-115715

EN219	E1/E2/E3 Enzyme	Cancer
EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC₅₀ of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination .

HY-134184

AUTAC2	AUTACs Autophagy	Inflammation/Immunology Cancer
AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. SLF binds non-covalently to FKBP12 .

HY-141550

BPK-25	Others	Inflammation/Immunology
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .

HY-161242

CBI1	Bcl-2 Family	Cancer
CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .

HY-149933

AM841	Cannabinoid Receptor	Neurological Disease
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .

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-122054

BPK-29	Others	Cancer
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells .

HY-122054A

BPK-29 hydrochloride	Others	Cancer
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells .

HY-100848

TX1-85-1 1 Publications Verification	EGFR	Cancer
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC₅₀ of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .

HY-158008

(R)-G12Di-7	Ras	Cancer
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .

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 2 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 .

Cat. No.	Product Name	Type

HY-D2270

Halo tag TMR	Fluorescent Dyes/Probes
Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and high affinity .

Cat. No.	Product Name

HY-K0225

Carboxyl Magnetic Beads (200 nm, 10 mg/mL)
MCE Carboxyl Magnetic beads (200 nm, 10 mg/mL) are characterized by superparamagnetism, fast magnetic response, abundant carboxyl functional groups, monodispersity, and submicron scale particle size. Biological ligands (proteins, peptides, oligonucleotides, drug molecules, etc.) can be covalently coupled to the surface of microspheres under the action of special chemical reagents (such as EDC).

Carboxyl Magnetic Beads (200 nm, 10 mg/mL)

MCE Carboxyl Magnetic beads (200 nm, 10 mg/mL) are characterized by superparamagnetism, fast magnetic response, abundant carboxyl functional groups, monodispersity, and submicron scale particle size. Biological ligands (proteins, peptides, oligonucleotides, drug molecules, etc.) can be covalently coupled to the surface of microspheres under the action of special chemical reagents (such as EDC).

Cat. No.	Product Name		Classification

HY-151716

Halo-DBCO		DBCO
Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples.

HY-115715A

EN219-alkyne		Alkynes
EN219-alkyne is an alkyne-functionalized EN219 probe. EN219 (HY-P0287A) is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC₅₀ of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination . EN219-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Fluorescent Dye

MCE Kits

Click Chemistry

Name
Email *

	Sorry, but the email address you supplied was invalid.