Classical Inhibitors

By Targets:	Apoptosis (2) Bacterial (1) Complement System (4) Formyl Peptide Receptor (FPR) (1) HIV (2) HIV Protease (1) HSP (1) Pim (1) PKC (1) Topoisomerase (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Infection (4) Inflammation/Immunology (5) Metabolic Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P990091

Riliprubart SAR 445088	Complement System	Inflammation/Immunology
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .

HY-108605

PIM1-IN-2	Pim	Cancer
PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a K_i of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds .

HY-120548

KBU2046	HSP	Cancer
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life .

HY-P1436

Acetyl-pepstatin

HIV Infection

Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR K_i values of 712 nM and 13 nM .
HY-146753

HIV-1 inhibitor-20

HIV Infection

HIV-1 inhibitor-20 is a potent HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles .

Acetyl-pepstatin	HIV	Infection
Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR K_i values of 712 nM and 13 nM .

HIV-1 inhibitor-20	HIV	Infection
HIV-1 inhibitor-20 is a potent HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles .

HY-145686

AV023	Others	Inflammation/Immunology
AV023 is a potent inhibitor of ANKRD22. AV023 promotes the expansion of gastrointestinal mucosal epithelial stem cells and indirectly activates the Wnt classical pathway, which helps the recovery of damaged gastrointestinal mucosal tissues in the body (extracted from patent CN111205231B) .

HY-163399

Antibacterial agent 197	Bacterial	Infection
Antibacterial agent 197 (compound 1-deAA) is a termination inhibitor of non-classical anhydroglycosyl receptors and anhydrowall peptide-type peptidoglycan (PG) in bacterial TGase, with activity against Staphylococcus aureus. Antibacterial agent 197 synergizes with Vancomycin (HY-B0671) and is its antibacterial adjuvant .

HY-146189

Topoisomerase II inhibitor 9	Topoisomerase Apoptosis	Cancer
Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC₅₀ of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC₅₀ of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells .

HY-P1036

Compstatin 1 Publications Verification	Complement System	Others
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1036A

Compstatin TFA 1 Publications Verification	Complement System	Others
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-N2996

Ganodermanondiol	HIV Protease	Infection
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum .Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC₅₀ of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC₅₀ of 41.7μM .

HY-P5469

WRW4-OH	Formyl Peptide Receptor (FPR)	Others
WRW4-OH is a biological active peptide. (This peptide inhibits binding of one of formyl peptide receptor-like 1 (FPRL1) agonists WKYMVm to its specific receptor. FPRL1 is an important classical chemoattractant receptor that is expressed in phagocytic cells in the peripheral blood and brain. Activation of FPRL1 is closely related to inflammatory responses in the host defense mechanism and neurodegenerative disorders.)

HY-117800

BJE6-106 1 Publications Verification B106	PKC Apoptosis	Inflammation/Immunology Cancer
BJE6-106 (B106) is a potent, selective 3 ^rd generation PKCδ inhibitor with an IC₅₀ of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC₅₀=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.

HY-P99965

Crovalimab SKY59; RO7112689	Complement System	Cardiovascular Disease Metabolic Disease
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .

Cat. No.	Product Name	Target	Research Area

HY-P1036

Compstatin 1 Publications Verification	Complement System	Others
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1036A

Compstatin TFA 1 Publications Verification	Complement System	Others
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .

HY-P1436

Acetyl-pepstatin

HIV Infection

Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR K_i values of 712 nM and 13 nM .

Acetyl-pepstatin	HIV	Infection
Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR K_i values of 712 nM and 13 nM .

HY-P5469

WRW4-OH	Formyl Peptide Receptor (FPR)	Others
WRW4-OH is a biological active peptide. (This peptide inhibits binding of one of formyl peptide receptor-like 1 (FPRL1) agonists WKYMVm to its specific receptor. FPRL1 is an important classical chemoattractant receptor that is expressed in phagocytic cells in the peripheral blood and brain. Activation of FPRL1 is closely related to inflammatory responses in the host defense mechanism and neurodegenerative disorders.)

Cat. No.	Product Name	Target	Research Area

HY-P990091

Riliprubart SAR 445088	Complement System	Inflammation/Immunology
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .

HY-P990025

Empasiprubart ARGX-117	Inhibitory Antibodies	Inflammation/Immunology
Empasiprubart (ARGX-117) a humanized inhibitory monoclonal antibody against complement C2. Empasiprubart prevents the formation of the C3 proconvertase and inhibits classical and lectin pathway activation upstream of C3 activation through binding to the Sushi-2 domain of C2. Empasiprubart exhibits pH- and calcium-dependent target binding. Empasiprubart prevents complement-mediated cytotoxicity in in vitro models for autoimmune hemolytic anemia and antibody-mediated rejection of organ transplants .

HY-P99965

Crovalimab SKY59; RO7112689	Complement System	Cardiovascular Disease Metabolic Disease
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .

HY-P990061

Polzastobart JTX 8064	Inhibitory Antibodies	Inflammation/Immunology
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2996

Ganodermanondiol	Infection Triterpenes Structural Classification Microorganisms Classification of Application Fields Terpenoids Polyporaceae Source classification Plants Disease Research Fields	HIV Protease
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum .Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC₅₀ of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC₅₀ of 41.7μM .

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Classical Inhibitors

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