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" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) Adenosine Receptor (1) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (11) Autophagy (9) Btk (1) c-Fms (1) c-Met/HGFR (2) Calcium Channel (2) CD3 (1) CGRP Receptor (1) Cytochrome P450 (1) Dihydrofolate reductase (DHFR) (1) Dopamine Receptor (2) Endonuclease (1) FKBP (1) GABA Receptor (1) GSK-3 (3) HDAC (2) Histone Demethylase (1) Interleukin Related (2) Isotope-Labeled Compounds (2) JAK (4) Lipoxygenase (1) mAChR (1) MEK (1) Mineralocorticoid Receptor (3) Monoamine Oxidase (2) Monocarboxylate Transporter (1) mTOR (2) Na+/H+ Exchanger (NHE) (2) Neuropeptide Y Receptor (2) NF-κB (2) NO Synthase (2) Orthopoxvirus (1) Oxytocin Receptor (1) P2X Receptor (2) P2Y Receptor (2) p38 MAPK (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (2) Potassium Channel (3) PPAR (1) Ras (1) Reactive Oxygen Species (1) ROR (2) SARS-CoV (1) Ser/Thr Protease (1) Sirtuin (1) Sodium Channel (2) TAM Receptor (1) Tie (1) TNF Receptor (2) Toll-like Receptor (TLR) (1) TRP Channel (1) VEGFR (5)
By Research Areas:	Cancer (36) Cardiovascular Disease (8) Endocrinology (1) Infection (5) Inflammation/Immunology (17) Metabolic Disease (7) Neurological Disease (17)

By Targets:

11β-HSD (1)

Adenosine Receptor (1)

Angiotensin-converting Enzyme (ACE) (1)

Apoptosis (11)

Autophagy (9)

Btk (1)

c-Fms (1)

c-Met/HGFR (2)

Calcium Channel (2)

CD3 (1)

CGRP Receptor (1)

Cytochrome P450 (1)

Dihydrofolate reductase (DHFR) (1)

Dopamine Receptor (2)

Endonuclease (1)

FKBP (1)

GABA Receptor (1)

GSK-3 (3)

HDAC (2)

Histone Demethylase (1)

Interleukin Related (2)

Isotope-Labeled Compounds (2)

JAK (4)

Lipoxygenase (1)

mAChR (1)

MEK (1)

Mineralocorticoid Receptor (3)

Monoamine Oxidase (2)

Monocarboxylate Transporter (1)

mTOR (2)

Na+/H+ Exchanger (NHE) (2)

Neuropeptide Y Receptor (2)

NF-κB (2)

NO Synthase (2)

Orthopoxvirus (1)

Oxytocin Receptor (1)

P2X Receptor (2)

P2Y Receptor (2)

p38 MAPK (1)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

PI3K (2)

Potassium Channel (3)

PPAR (1)

Ras (1)

Reactive Oxygen Species (1)

ROR (2)

SARS-CoV (1)

Ser/Thr Protease (1)

Sirtuin (1)

Sodium Channel (2)

TAM Receptor (1)

Tie (1)

TNF Receptor (2)

Toll-like Receptor (TLR) (1)

TRP Channel (1)

VEGFR (5)

By Research Areas:

Cancer (36)

Cardiovascular Disease (8)

Endocrinology (1)

Infection (5)

Inflammation/Immunology (17)

Metabolic Disease (7)

Neurological Disease (17)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Axatilimab SNDX-6352	c-Fms	Inflammation/Immunology Cancer
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .

Tonapofylline BG 9928	Adenosine Receptor	Cardiovascular Disease Metabolic Disease
Tonapofylline (BG 9928) is an orally active and selective adenosine A₁ receptor antagonist with a K_i of 7.4 nM for human adenosine A₁ receptor (hA₁), which displays 915-fold selectivity versus human adenosine A_2A receptor and 12-fold selectivity versus human adenosine A_2B receptor and is used in development for the treatment of heart failure .

AR-C141990 hydrochloride	Monocarboxylate Transporter	Inflammation/Immunology
AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pK_i values of 7.6, 6.6 for MCT-1 and MCT-2, respectively . AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response .

Mpro/PLpro-IN-1	SARS-CoV	Infection
Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M ^pro/PL ^pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M ^pro (IC₅₀ = 1.72 μM) and submicromolar potency versus PL ^pro (IC₅₀ = 0.67 μM) .

Panadiplon FG 10571; PNU 78875	GABA Receptor	Neurological Disease
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .

DHFR-IN-11	Dihydrofolate reductase (DHFR)	Infection
DHFR-IN-11 (compound 6b) is inhibitor of DHFR, and has inhibitory potency versus M. tuberculosis DHFR enzyme with IC₅₀ values 5.70 μM .

CS12192	Others	Others
CS12192 is a compound improving survival and weight gain. CS12192 has the potential for the research of graft-versus-host disease (GVHD) (extracted from the patent CN112773802A) .

VX-702 3 Publications Verification	p38 MAPK Autophagy	Inflammation/Immunology
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β .

MK-3207 Hydrochloride 3 Publications Verification	CGRP Receptor	Neurological Disease
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

(+)-KCC2 blocker 1	Potassium Channel	Neurological Disease
(+)-KCC2 blocker 1 is a selective K ⁺-Cl ^- cotransporter KCC2 blocker with an IC₅₀ of 0.4 μM. (+)-KCC2 blocker 1 is a benzyl prolinate and a enantiomer of KCC2 blocker 1 .

KCC2 blocker 1	Potassium Channel	Neurological Disease
KCC2 blocker 1 is an orally active and selective K ⁺-Cl ^- cotransporter KCC2 blocker with an IC₅₀ of 1 μM. KCC2 blocker 1 is a benzyl prolinate .

Momelotinib Mesylate CYT387 Mesylate	JAK Autophagy	Cancer
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.

SGX-523 5+ Cited Publications	c-Met/HGFR	Cancer
SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC₅₀ of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .

PSB-1491	Monoamine Oxidase	Neurological Disease
PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC₅₀ of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .

PFM01	Endonuclease	Cancer
PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR) .

Elastatinal
Elastatinal is a potent and competitive inhibitor of elastase, with a K_i of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .

Inolimomab	Interleukin Related	Inflammation/Immunology
Inolimomab is an anti-interleukin-2 receptor (IL-2R) α chain monoclonal antibody. Inolimomab improves the survival rate in the early research of treating acute graft-versus-host disease (aGVHD) .

Momelotinib sulfate 10+ Cited Publications CYT387 sulfate salt	JAK Autophagy Apoptosis	Cancer
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

BRD9757	HDAC	Cancer
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC₅₀ of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs .

GW 590735	PPAR	Metabolic Disease
GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC₅₀=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia .

MLN-4760 10+ Cited Publications	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
MLN-4760 is a potent and selective human ACE2 inhibitor (IC₅₀, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC₅₀, >100 μM) and bovine carboxypeptidase A (CPDA; IC₅₀, 27 μM).

NaV1.7 inhibitor-1	Sodium Channel	Neurological Disease
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC₅₀ of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5 .

Ruxolitinib sulfate INCB018424 sulfate	JAK Autophagy	Cancer
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC₅₀s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.

Enpp-1-IN-17	Phosphodiesterase (PDE)	Infection Cancer
Enpp-1-IN-17 (example 274) is a potent ENPP1 inhibitor, with the inhibition constants (Ki values) toward cGAMP and ATP hydrolysis of 100 nM-1 μM and > 1 μM, respectively. The selectivity ratio for inhibition of cGAMP hydrolysis versus ATP hydrolysis is >6.4 .

(Rac)-Finerenone (Rac)-BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .

Neihulizumab ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab)	Apoptosis	Inflammation/Immunology
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .

WYE-132 5+ Cited Publications WYE-125132	mTOR Apoptosis	Cancer
WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC₅₀: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.

Osthenol Ostenol	Monoamine Oxidase	Neurological Disease
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (K_i=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC₅₀ of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .

PD 168568 dihydrochloride	Dopamine Receptor	Neurological Disease Cancer
PD 168568 dihydrochloride is a orally active and potent dopamine receptor D₄ (DRD₄) antagonist. PD 168568 dihydrochloride contains an isoindolinone and is selective for the D₄ receptor versus D₂ and D₃, with K_i values of 8.8, 1842, and 2682 nM, respectively. PD 168568 dihydrochloride can be used for glioblastoma (GBM) research .

Cavα2δ-IN-1	Calcium Channel	Others
Cavα2δ-IN-1 shows high selectivity for voltage-gated calcium channels Cavα2δ-1 (K_i 6 nM) versus Cavα2δ-2 (K_i ＞ 10000 nM).

PD 168568	Dopamine Receptor	Neurological Disease Cancer
PD 168568 is a orally active and potent dopamine receptor D₄ (DRD₄) antagonist. PD 168568 contains an isoindolinone and is selective for the D₄ receptor versus D₂ and D₃, with K_i values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research .

Dafsolimab SPV-T3a	CD3	Infection
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .

SRT 1460 1 Publications Verification	Sirtuin	Cancer
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC_1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues .

BRD0705 1 Publications Verification	GSK-3	Cancer
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC₅₀ of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .

Cligosiban 5 Publications Verification PF-3274167	Oxytocin Receptor	Endocrinology
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (K_i=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V_1b and V_1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .

GDC-0623 5+ Cited Publications RG 7421; MEK inhibitor 1	MEK Apoptosis	Cancer
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (K_i=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC₅₀=42 nM) versus A375 (BRAF ^V600E, EC₅₀=7 nM).

BI-749327 10+ Cited Publications	TRP Channel	Cardiovascular Disease
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC₅₀s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .

PSB-1114 tetrasodium	P2Y Receptor	Metabolic Disease
PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y₂ receptor agonist with an EC₅₀ of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y₄ (EC₅₀ of 9.3 μM) and P2Y₆ (EC₅₀ of 7.0 μM) receptors .

PSB-1114 triethylamine	P2Y Receptor	Cancer
PSB-1114 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y₂ receptor agonist with an EC₅₀ of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y₄ (EC₅₀ of 9.3 μM) and P2Y₆ (EC₅₀ of 7.0 μM) receptors .

hnNOS-IN-3	NO Synthase	Neurological Disease
hnNOS-IN-3 (compound 39) is a selective nNOS inhibitor, with a K_i of 0.32 μM. The nNOS binding of hnNOS-IN-3 is competitive with L-arginine. The selectivity of hnNOS-IN-3 for nNOS versus iNOS (K_i=37 μM) and eNOS (K_i=9.4 μM) is 115-fold and 29-fold, respectively .

Vandetanib 15+ Cited Publications ZD6474	VEGFR Autophagy Apoptosis	Cancer
Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM) .

Vandetanib hydrochloride ZD6474 hydrochloride	VEGFR Autophagy Apoptosis	Cancer
Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM) .

Vandetanib trifluoroacetate ZD6474 trifluoroacetate	VEGFR Autophagy Apoptosis	Cancer
Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM) .

IT-901	NF-κB	Cancer
IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC₅₀ of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD) .

2-Aminoquinoline 2-Quinolinamine	NO Synthase Orthopoxvirus	Infection Neurological Disease
2-Aminoquinoline (2-Quinolinamine) is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline exhibits antiviral activity against the vaccinia virus. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents .

Daminozide 2 Publications Verification	Histone Demethylase	Cancer
Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC₅₀s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .

Cat. No.	Product Name	Target	Research Area

HY-P4667

VLHDDLLEA	Peptides	Metabolic Disease
VLHDDLLEA is a peptide that can be isolated from the MHC complex HLA-A0201 molecule. VLHDDLLEA can be recognized by HLA-A0201-restricted cytotoxic T cells (CTLs). VLHDDLLEA can be used for research on graft versus host disease (GvHD) .

Cat. No.	Product Name	Target	Research Area

HY-P99452

Axatilimab SNDX-6352	c-Fms	Inflammation/Immunology Cancer
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .

HY-P99664

Inolimomab	Interleukin Related	Inflammation/Immunology
Inolimomab is an anti-interleukin-2 receptor (IL-2R) α chain monoclonal antibody. Inolimomab improves the survival rate in the early research of treating acute graft-versus-host disease (aGVHD) .

HY-P99378

Neihulizumab ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab)	Apoptosis	Inflammation/Immunology
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .

HY-P99636

Gavilimomab ABX-CBL	Inhibitory Antibodies	Inflammation/Immunology
Gavilimomab (ABX-CBL) is an IgM murine monoclonal antibody that recognizes CD147 on the cell surface and initiates cell killing through complement-mediated lysis. Gavilimomab can be used for the research of graft-versus-host disease (GVHD) .

HY-P99837

Dafsolimab SPV-T3a	CD3	Infection
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .

HY-P99445

Asunercept APG101; CAN008	TNF Receptor	Inflammation/Immunology Cancer
Asunercept (APG101; CAN008) is a soluble CD95-Fc fusion protein targeting CD95L. Asunercept disrupts CD95/CD95L signaling by selectively binding to CD95L. Asunercept can be used in the research of glioblastoma multiforme (GBM), myelodysplastic syndrome (MDS), and graft-versus-host disease (GvHD) .

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