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ternary complex

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Apoptosis (1) Bacterial (1) Cyclophilin (2) DNA/RNA Synthesis (1) E1/E2/E3 Enzyme (2) Epigenetic Reader Domain (3) ERK (1) FGFR (1) HDAC (1) Hexokinase (1) Ligands for E3 Ligase (2) MDM-2/p53 (1) Molecular Glues (6) mTOR (1) NAMPT (1) NF-κB (1) Notch (1) Nucleoside Antimetabolite/Analog (1) Phosphodiesterase (PDE) (1) PI3K (1) PROTACs (6) Ras (5) Thymidylate Synthase (1) Toll-like Receptor (TLR) (1)
By Research Areas:	Cancer (21) Infection (2) Neurological Disease (1)
Oligonucleotides:	Nucleosides and their Analogs (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Oligonucleotides

Targets Recommended: Arp2/3 Complex

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100431

IMR-1 5 Publications Verification	Notch	Cancer
IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC₅₀ of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth .

HY-162730

OPB-171775	Molecular Glues Phosphodiesterase (PDE)	Cancer
OPB-171775 is a molecular glue, which forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway, and exhibits antitumor efficacy .

HY-156401

BRD9 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
BRD9 Degrader-1 (Compound 13-7) is a PROTAC BRD9 degrader . BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062)。(Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) .

HY-162536

Pan-RAS-IN-5	Molecular Glues Cyclophilin Ras	Cancer
Pan-RAS-IN-5 (compound 7A) is a molecular glues that can form a ternary complex with the proteins cyclophilin A (CYPA) and RAS (ON). The formation of the ternary complex can block the binding of RAS downstream of RAF and has anti-tumor effects .

HY-158409

Pan-RAS-IN-2	Molecular Glues Ras Cyclophilin	Cancer
Pan-rasin-2 (compound 6A) is a molecular glues that targets RAS. Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor effects .

HY-123259

CB3731	Others	Others
CB3731 is an analogue of N-10-(fluoroethyl)quinazolinylfolate and can be used for fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase .

HY-159163

KRASG12C IN-12	Ras	Cancer
KRASG12C IN-12 (compound-1) is a KRAS ^G12C inhibitor. KRASG12C IN-12 (compound-1) can form a ternary complex with intracellular CYPA and the activated KRAS ^G12C mutant .

HY-168646

SJ46411-Br	Ligands for E3 Ligase	Cancer
SJ46411-Br is one of CRL2 ^KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs .

HY-W008341

5-Chloroisoquinoline	Toll-like Receptor (TLR)	Neurological Disease
5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration .

HY-156820

HLDA-221	Others	Cancer
HLDA-221 is a heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras (RIPTACs). HLDA-221 elicits a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival, thus leading to cell death selectively in cells expressing the target protein .

HY-152154

Nampt degrader-2	PROTACs NAMPT	Cancer
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC₅₀ of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD ⁺ and exerts potent antitumor activities .

HY-154508

FdUMP triethylammonium 2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium	Nucleoside Antimetabolite/Analog Thymidylate Synthase	Cancer
FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.

HY-122643

NITD-916	Bacterial	Infection
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC₅₀ of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects .

HY-163639

BRD4 degrader-2	Molecular Glues Epigenetic Reader Domain E1/E2/E3 Enzyme	Cancer
BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .

HY-152134

HDAC6 degrader-3	HDAC PROTACs	Cancer
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC₅₀ value of 19.4 nM. HDAC6 degrader-3 has IC₅₀s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin .

HY-49444

EN450	NF-κB Molecular Glues E1/E2/E3 Enzyme	Cancer
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .

HY-154992

2,4-Difluorophenylethynylcobalamin F2PhEtyCbl	Others	Others
2,4-Difluorophenylethynylcobalamin is a potential B12 antivitamin via binding to human B12 -processing enzyme CblC with high affinity (KD=130 nm). 2,4-Difluorophenylethynylcobalamin withstood tailoring by CblC, and stabilizes the ternary complex with the cosubstrate glutathione (GSH) . 2,4-Difluorophenylethynylcobalamin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-156671

RMC-4998	Ras PI3K ERK mTOR Apoptosis	Cancer
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS ^G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS ^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS ^G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .

HY-163168

aTAG 4531 CFT-4531	PROTACs DNA/RNA Synthesis	Cancer
aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC₅₀ value of 0.28 nM and K_i value of 1.8 nM. The degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader. Red: MTH1 aTAG inhibitor (HY-134725), Blue: CRBN ligand (HY-126457), Black: linker (HY-108374) .

HY-161841

Antitumor agent-177	FGFR	Cancer
Antitumor agent-177 (compound 57), a non-steroidal NSC12 derivative, shows potent FGF2 binding affinity with a K_d of 24 μM by SPR. Antitumor agent-177 significantly inhibits the formation of HSPG/FGF2/FGFR1 ternary complexes. Antitumor agent-177 inhibits FGFR activation and exerts a potent anti-tumor activity on multiple myeloma (MM) cell lines in vitro and in vivo .

HY-117730

Pulvomycin Antibiotic 1063Z	Antibiotic	Infection
Pulvomycin (Antibiotic 1063Z) is an antibiotic with protein biosynthesis inhibitory activity. Pulvomycin is able to block protein biosynthesis in Bacillus brevis grown in cells. Pulvomycin is highly sensitive to poly(Phe) synthesis in cell-free systems. Pulvomycin does not affect the transfer of phenylalanine to tRNA. Studies have shown that the target of Pulvomycin is the elongation of the polypeptide chain. Pulvomycin can also prevent the formation of a ternary complex between the elongation factor Tu, GTP and aminoacyl-tRNA .

HY-160695

PT-179	Ligands for E3 Ligase Molecular Glues	Cancer
PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .

HY-155356

YN14	PROTACs Ras	Cancer
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.

HY-155008

PROTAC HK2 Degrader-1 2 Publications Verification	Hexokinase	Cancer
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .

HY-168634

SJ46421	PROTACs Epigenetic Reader Domain	Cancer
SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC₅₀ of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)) .

HY-159606

MS182	MDM-2/p53	Cancer
MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53 ^Y220C stabilizer and targeting p53 ^Y220C. MS182 is composed of p53 ^Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53 ^Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53 ^Y220C (ACE₅₀: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI₅₀ values of 2.16 μM and 1.83 μM for BxPC3 (p53 ^Y220C/-) and NUGC (p53 ^Y220C/+), respectively .

Cat. No.	Product Name

HY-L137

Molecular Glue Compound Library	42 compounds
Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention. Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy. MCE supplies a unique collection of 42 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.

Molecular Glue Compound Library

42 compounds

Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.

Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.

MCE supplies a unique collection of 42 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-117730

Pulvomycin Antibiotic 1063Z	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Antibiotic
Pulvomycin (Antibiotic 1063Z) is an antibiotic with protein biosynthesis inhibitory activity. Pulvomycin is able to block protein biosynthesis in Bacillus brevis grown in cells. Pulvomycin is highly sensitive to poly(Phe) synthesis in cell-free systems. Pulvomycin does not affect the transfer of phenylalanine to tRNA. Studies have shown that the target of Pulvomycin is the elongation of the polypeptide chain. Pulvomycin can also prevent the formation of a ternary complex between the elongation factor Tu, GTP and aminoacyl-tRNA .

Cat. No.	Product Name		Classification

HY-154508

FdUMP triethylammonium 2’-Deoxy-5-Fluorouridine 5’-phosphate triethylammonium		Nucleosides and their Analogs
FdUMP triethylammonium is the intracellular active form of 5-fluorouracil (5-FU). 5-FU is converted to FdUMP after being transported into the cell by various enzymes. FdUMP forms a ternary complex with thymidylate synthase and its cofactor 5,10-methylene tetrahydrofolate, inhibiting the activity of thymidylate synthase, which in turn leads to the suppression of DNA synthesis.

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