Hybrid inhibitor

By Targets:	Amylases (1) Antibiotic (2) Apoptosis (2) Bacterial (5) Bcl-2 Family (1) Cannabinoid Receptor (1) Carbonic Anhydrase (1) COX (2) DNA/RNA Synthesis (1) Endogenous Metabolite (1) Farnesyl Transferase (1) Ferroptosis (1) Glucosidase (1) HDAC (3) HIF/HIF Prolyl-Hydroxylase (1) HIV (1) Keap1-Nrf2 (1) Lipoxygenase (1) Microtubule/Tubulin (2) NF-κB (1) p38 MAPK (1) Pim (1) ROCK (1) SphK (1) TRP Channel (1)
By Research Areas:	Cancer (9) Endocrinology (1) Infection (5) Inflammation/Immunology (3) Neurological Disease (3)
Click Chemistry:	Alkynes (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P3383A

Peceleganan acetate PL-5 acetate	Bacterial	Infection
Peceleganan (PL-5) acetate is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan acetate inhibits wound infection .

HY-144332

PHD2/HDACs-IN-1	HDAC HIF/HIF Prolyl-Hydroxylase	Cancer
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC₅₀s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI) .

HY-P5204

Enterocin Hybrid 1 K1-EJ Hybrid	Bacterial	Infection
Enterocin Hybrid 1 is a antibacterial agent, a antibacterial composition. Enterocin Hybrid 1 inhibits Vancomycin (HY-B0671)-resistant E. faecium, Staphylococcus haemoliticus .

HY-P3383

Peceleganan PL-5	Bacterial	Infection
Peceleganan (PL-5) is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan inhibits wound infection .

HY-107164

Thiomarinol A 4-Hydroxythiomarinol C	Antibiotic Bacterial	Infection
Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a K_i ^app value of 19 nM .

HY-N11880

2-O-Sinapoyl makisterone A	COX	Cancer
2-O-Sinapoyl makisterone A (compound 2), a sinapinic acid-ecdysterone hybrid, is a selective inhibitor of COX-2. 2-O-Sinapoyl makisterone A significantly inhibits the expression of COX-2 protein .

HY-19738

NQTrp
NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide ( ⁴¹GCWMLY ⁴⁶ within the N-terminus of γD-crystallin) as well as full-length γD-crystallin .

HY-115970

Tubulin inhibitor 21	Microtubule/Tubulin	Cancer
Tubulin inhibitor 21 (compound 6f), a chalcone- and melatonin- based hybrid, is a potent tubulin inhibitor. Tubulin inhibitor 21 induces a remarkable cytotoxic activity toward SW480 cells (IC₅₀=0.26 μM) with lower effect against nonmalignant cells .

HY-151351

SphK2-IN-2

SphK Cancer

SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC₅₀ value of 0.23 μM .

SphK2-IN-2	SphK	Cancer
SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC₅₀ value of 0.23 μM .

HY-P35433

Tifuvirtide T-1249	HIV	Inflammation/Immunology
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection .

HY-162170

Anti-inflammatory agent 72	NF-κB Keap1-Nrf2 p38 MAPK	Inflammation/Immunology
Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways .

HY-149016

Tubulin polymerization-IN-25	Microtubule/Tubulin Farnesyl Transferase	Cancer
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC₅₀s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .

HY-131678

Palmitoyl serotonin PA-5HT	Others	Neurological Disease
Palmitoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin, antagonist of FAAH. Palmitoyl serotonin inhibits L-3,4-dihydroxyphenylalanine (HY-N0304) induced abnormal involuntary movements. Palmitoyl serotonin has the potential for the research of parkinson's disease (PD) .

HY-115999

Carbonic anhydrase inhibitor 12	Carbonic Anhydrase	Cancer
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (K_is of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines .

HY-135184

Rifaquizinone CBR-2092; TNP-2092	Antibiotic Bacterial DNA/RNA Synthesis	Infection
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC₅₀ of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci .

HY-135882

OMDM-6	TRP Channel Cannabinoid Receptor Endogenous Metabolite	Neurological Disease
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC₅₀=75 nM) and cannabinoid receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM .

HY-143233

PIM-1/HDAC-IN-1	Pim HDAC Apoptosis	Cancer
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC₅₀ of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC₅₀ values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .

HY-163188

COX-2/LOX-IN-2	COX Lipoxygenase	Inflammation/Immunology
COX-2/LOX-IN-2 (compound 6) is a dual inhibitor of COX-2/LOX with IC₅₀s of 7.0 μM and 27.5 μM, respectively. COX-2/LOX-IN-2 has antioxidant activity and has the potential to be used in the development of nonsteroidal anti-inflammatory drugs (tNSAIDs) .

HY-151872

HDAC-IN-48	HDAC Ferroptosis	Cancer
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI₅₀~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 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-145294

ROCK2-IN-5	ROCK	Neurological Disease
ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .

HY-162390

α-Amylase/α-Glucosidase-IN-11	Amylases Glucosidase	Endocrinology
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC₅₀ = 30.39 μM) and α-glucosidase (IC₅₀ = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .

HY-149009

Bcl-2-IN-9	Bcl-2 Family Apoptosis	Cancer
Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC₅₀ value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells .

Cat. No.	Product Name	Target	Research Area

HY-P3383A

Peceleganan acetate PL-5 acetate	Bacterial	Infection
Peceleganan (PL-5) acetate is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan acetate inhibits wound infection .

HY-P5204

Enterocin Hybrid 1 K1-EJ Hybrid	Bacterial	Infection
Enterocin Hybrid 1 is a antibacterial agent, a antibacterial composition. Enterocin Hybrid 1 inhibits Vancomycin (HY-B0671)-resistant E. faecium, Staphylococcus haemoliticus .

HY-P3383

Peceleganan PL-5	Bacterial	Infection
Peceleganan (PL-5) is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan inhibits wound infection .

HY-P35433

Tifuvirtide T-1249	HIV	Inflammation/Immunology
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-107164

Thiomarinol A 4-Hydroxythiomarinol C	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	Antibiotic Bacterial
Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a K_i ^app value of 19 nM .

HY-N11880

2-O-Sinapoyl makisterone A	Structural Classification Source classification Fibraurea recisa Pierre Plants Menispermaceae Steroids	COX
2-O-Sinapoyl makisterone A (compound 2), a sinapinic acid-ecdysterone hybrid, is a selective inhibitor of COX-2. 2-O-Sinapoyl makisterone A significantly inhibits the expression of COX-2 protein .

HY-135882

OMDM-6	Structural Classification Alkaloids Monophenols Neurological Disease Classification of Application Fields Other Alkaloids Source classification Phenols Endogenous metabolite Disease Research Fields	TRP Channel Cannabinoid Receptor Endogenous Metabolite
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC₅₀=75 nM) and cannabinoid receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM .

Cat. No.	Product Name		Classification

HY-151872

HDAC-IN-48		Alkynes
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI₅₀~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Hybrid inhibitor

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