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SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with IC50=2.3 μM that has inhibitory activity through SIRT5-dependent deacetylation and can be used to study cancer and neurodegenerative diseases.

SKF96067 is a reversible gastric H+/K+-ATPase inhibitor that can induce relaxation of human airway smooth muscle in vitro.

ABP-102 (CT P72) is a tetravalent IgG1-[L]-scFv bispecific t-cell adduct (BiTE) that acts as a CD3 modulator and selective HER2 modulator for the selective targeting of HER2 overexpressing tumors. ABP-102 showed cytotoxicity in HER2-overexpressing models of breast and gastric cancers, while significantly decreasing activity against HER2 low level cells, twice as effective as rununmotamab.

CEP-9722 is an orally active, selective and potent inhibitor of poly (ADP-ribose) polymerase-1 PARP-1 and poly (ADP-ribose) polymerase-12 PARP-2, with anticancer activity, and can be used for the study of ovarian cancer.

IMB-XMA0038 is a novel inhibitor targeting Mycobacterium tuberculosis aspartate semialdehyde dehydrogenase with antimicrobial activity for use in tuberculosis research.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

ZTZ240 is a KCNQ2 channel activator used in the study of epilepsy.

PF-06647263 (anti-EFNA4-ADC) is an ADC compound targeting EFNA4, with anti-tumor activity, composed of an anti-EFNA4 antibody conjugated with calicheamicin, inducing significant tumor regression in TNBC xenografts.

BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes.

GSK4418959 (IDE275) is a non-covalent, reversible, selective, and orally active inhibitor of the Werner syndrome helicase (WRN helicase). GSK4418959 inhibits both ATPase and DNA unwinding activities of WRN helicase in an ATP-competitive manner. GSK4418959 is a valuable chemical tool for the study of microsatellite instability-high (MSI-H) cancers, where WRN helicase plays an essential role in maintaining genomic stability.

HTT-D3 is an orally active, highly efficient Huntington splicing modulator. It induces HTT mRNA degradation, reduces HTT protein levels, and inhibits P-glycoprotein (P-gp) efflux. This compound can be used in Huntington's disease research.

Leritrelvir (RAY1216) is an orally active and highly potent protease inhibitor with antiviral activity that blocks cleavage of viral precursor proteins and inhibits viral replication in SARS-CoV-2.

Anti-Mouse PD-1 Antibody (RMP1-14) is an IgG2a antibody inhibitor against mouse PD-1 and can block PD-1/PD-L1 signaling.

(Rac)-Modipafantis an orally available and selective platelet-activating factor receptor (PAFR) antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits, and can be used to study arthritis and ischemia/reperfusion (I/R) in the superior mesenteric artery (SMA) of the rat.

SU 10603 is a specific inhibitor of 17α-hydroxylase (also known as CYP17A1 and P450c17) used to study steroid hormone synthesis.

CYP1B1-IN-1 is a selective and highly potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.

CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.

GDC-2992 is a selective and orally active androgen receptor (AR) degradator that degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, making it suitable for studying castration-resistant prostate cancer (CRPC).

AGN 205327 is a potent synthetic agonist of retinoic acid receptors (RARs), with EC50 values of 3766 nM for RARα, 734 nM for RARβ, and 32 nM for RARγ, and AGN 205327 demonstrates no inhibitory activity against retinoid X receptors (RXRs), thereby exhibiting selective receptor subtype targeting that makes AGN 205327 an important tool for probing retinoid signaling pathways and investigating therapeutic applications of RAR activation.

p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes hypothermia induced by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and can be used to study neurological diseases.

YB-0158 ammonium (Wnt pathway inhibitor 2 ammonium) is a reverse-rotation peptidomimetic small molecule with translation-enhancing potential and anticancer activity. YB-0158 ammonium disrupts Sam68-Src interaction and induces apoptosis in colorectal cancer cells, which can be used to study cancer.

Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody targeting plasma kallikrein (pKal) with a Ki value of 0.12 nM. Lanadelumab effectively inhibits both free pKal and its interaction with high molecular weight kininogen (HMWK)-bound pKal. Lanadelumab has demonstrated potential in hereditary angioedema research and represents a promising therapeutic antibody for studying kallikrein-kinin system regulation.

DCC-3116 is an orally active, selective and potent ULK1/2 inhibitor with anticancer activity.DCC-3116 inhibits autophagy and can be used in cancer research.

Gimsilumab (MORAb-022) is a humanized monoclonal antibody targeting granulocyte macrophage colony-stimulating factor for the study of COVID-19-induced inflammation and hypoxemia.

NBD-PE is a lipid dye used primarily as a probe to study lipid organisation and dynamics within cell membranes and also to study membrane fusion by fluorescence resonance energy transfer (FRET), Ex=463 nm, Em=536 nm.

ICSN3250 HCl is an mTOR inhibitor that specifically targets cancer cells, competing with and displacing phosphatidic acid in the FRB structural domain of mTOR, thereby preventing mTOR activation and leading to cytotoxicity.

ABBV-969 Payload (Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT) is a drug-linker conjugate employed in the synthesis of antibody-drug conjugates (ADCs). The ABBV-969 Payload contains a Topoisomerase I inhibitor molecule and a chemical linker, enabling coupling with anti-c-Met antibodies to generate ABBV-969 ADCs with targeted anticancer activity.

SAR-114137 is a histone sphingomyelin kinase inhibitor used in the study of molluscum arteriosum and peripheral neuropathic pain.

GW 583340 dihydrochloride is a potent and orally available dual EGFR/ErbB2 (epidermal growth factor receptor/tyrosine kinase) inhibitor and is capable of reversing ABCG2- and ABCB1-mediated resistance.GW 583340 dihydrochloride selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, and inhibits 80% of tumor growth in a mouse xenograft model, with potential anticancer activity.

Lemuteporfin is a light-activated photosensitizing agent that is rapidly internalized by viable cells, localizing within the cytoplasm and associating with mitochondria. This localization is a key characteristic that confers strong cytotoxic potential upon light activation. Lemuteporfin has demonstrated the ability to reduce sebaceous gland volume in preclinical animal studies. It is currently under investigation in relation to benign prostatic hyperplasia and in topical form for the management of androgenetic alopecia.

PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.

AKP-001 is a selective inhibitor of MAPK of the p38α isoform and is used in the study of immune and digestive disorders.

AS-136A is an orally active measles virus RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that inhibits measles virus and blocks viral RNA synthesis.

Valomaciclovir stearate (A-174606. 0) is a nucleoside analog with antiviral activity against varicella-zoster virus (VZV), and has been used in the study of VZV infections.

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

Solenopsin HCl is an alkaloid extracted from fire ants, inhibiting phosphoinositide 3-kinase signaling and angiogenesis in a dose-dependent manner, affecting cardiovascular function, and used in cardiovascular disease research.

Trimethylcolchicinic acid (N-Deacetylcolchiceine) is an orally available colchicine analog that binds to tubulin and inhibits its polymerization into microtubules, preventing cell division and having potential antitumor activity.

M0324 is a novel MUC-1 conditional CD40 agonist composed of an anti-MUC-1 IgG and two identical CD40-targeting camelid VHH domains, designed to selectively activate immune cells in the context of tumor cells with high MUC-1 expression.

5-OP-RU is a MAIT-activating ligand, the major antigen of MAIT cells, a mucosal adjuvant, induces efficient enrichment of mucosal-associated invariant T cells, and can be used to study Mycobacterium tuberculosis infections.

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

Lodelaben (Declaben, SC-39026) is a reversible, non-competitive inhibitor of human neutrophil elastase (HNE), characterized by specificity and potency (IC50=0.5 μM, Ki=1.5 μM).

KLS-13019 is a highly effective and orally active GPR55 receptor antagonist, a cannabidiol (CBD)-derived neuroprotective agent that can reverse chemotherapy-induced peripheral neuropathy (CIPN) and is suitable for studying hepatic encephalopathy (HE).

BRD4884 is a highly selective and efficient HDAC1 and HDAC2 inhibitor that also inhibits HDAC3, used in research on neurological disorders.

RIPK2-IN-3 (FCG806791773) is a receptor-interacting serine/threonine protein kinase 2 (RIPK2) inhibitor with anti-inflammatory and anti-tumor activity. It can be used for research on immune diseases and cancer.

AZD0022 is a selective and orally active KRAS G12D inhibitor that displays exposure-dependent pRSK inhibition in a GP2D xenograft model.

LRH-1 Inhibitor-3 is an antagonist that inhibits LRH-1 transcriptional activity, reducing the expression of target genes associated with cell growth and proliferation, such as SHP (small heterodimer partner), cyclin E1 (CCNE1), and G0S2, and inhibiting the proliferation of human pancreatic, colon, and breast adenocarcinoma cells.

(R)-DOI hydrochloride is a potent 5-HT2A and 5-HT2C receptor agonist, orally active and capable of producing hallucinogenic effects.

IACS-52825 is a selective and potent dual leucine zipper kinase (DLK) inhibitor that reverses para-mechanical aberrant pain in a CIPN mouse model for the study of neurological disorders.

Vaniprevir is a non-covalent competitive HCV NS3/4A protease inhibitor, an antiviral drug that acts directly on the hepatitis C virus. Vaniprevir blocks the viral replication process by inhibiting the activity of HCV NS3/4A protease.

ReN-1869 is a novel selective histamine H(1) receptor antagonist with anti-neurogenic pain and anti-inflammatory activity for the study of neurological diseases.

PF-07328948 is a branched-chain keto acid dehydrogenase kinase (BDK) inhibitor, useful in research on cardiovascular disease (CVD) and metabolic disorders.

Laromustine (VNP40101M) is a sulfonyl hydrolytic alkylating prodrug used in cancer therapy with significant anticancer activity. Inhibiting thioredoxin reductase can be used to study acute myeloid leukemia.

DX3-234 is a potent oxidative phosphorylation (OXPHOS) inhibitor that acts by inhibiting complex I in the mitochondrial electron transport chain (ETC), leading to intracellular ATP depletion and cell death, and can be used for the treatment of specific cancers dependent on aerobic metabolism, such as pancreatic cancer.

STX-107 is a potent and selective mGluR5 agonist for the study of Fragile X Syndrome.

SMA-12b is an analog of the immunomodulatory parasite product ES-62 that has immunomodulatory activity, can modify the expression of many inflammatory response genes, increase the expression of many genes related to antioxidant responses, and can be used in the study of rheumatoid arthritis (RA) and other autoimmune diseases.

SB 216641 hydrochloride (SB-216641A) is a selective 5-HT1B/D receptor antagonist with anxiolytic properties that antagonizes the vasoconstrictor response mediated by sumatriptan. 10-O-Methylprotosapphosporin is an HbF inducer that can be used in the study of metabolic disorders and diabetes.

PBRM (17β-HSD1-IN-2) is a selective covalent inhibitor of 17β-HSD1, used in breast cancer and endometriosis research.

Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) that inhibits HIV replication by inhibiting HIV-1 reverse transcriptase activity and preventing the transcription of viral RNA into DNA for use in Highly Active Antiretroviral Therapy (HAART) programs and HIV disease studies

GSK-7227, a novel compound representing a novel class of peroxisome proliferator-activated receptor delta (PPARδ) partial agonists, demonstrates potent partial agonistic activity by upregulating the expression of PPARδ target genes, specifically carnitine palmitoyltransferase 1a (CPT1a) and pyruvate dehydrogenase kinase 4 (PDK4), in cultured skeletal muscle cells, indicating its potential role in modulating skeletal muscle metabolism and energy homeostasis.

RLX (PD 139530) is a PI3K/Akt/FoxO3a signal inhibitor with anticancer activity against tumour cell lines such as colon cancer, inducing sub-G1 arrest and mitochondrial potential loss, thereby inhibiting tumour growth. RLX also exhibits antitussive and anti-asthmatic activity, reducing eosinophils and total lymphocytes in bronchoalveolar lavage (BAL) fluid, and exhibits toxicity toward A549 cells.

HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.

Factor B-IN-5 is a complement factor B inhibitor, which can be used to study immune-related diseases.

RMC5127 is an oral and mutation-selective inhibitor of RASG12V (ON) that inhibits the GTP-bound (ON) form of RAS G12V through the formation of a high-affinity triplex with central nervous system (CNS) permeability and brain permeability. RMC5127 inhibits RAS pathway activity in vitro in KRAS G12V mutant human cancer cells and cellular proliferation, and antitumor activity in preclinical intracranial xenograft models and subcutaneous CDX and PDX models of KRAS G12V mutant NSCLC, PDAC and CRC.

GCN2-IN-7 is an orally active, potent and selective inhibitor of the environmental sensing protein GCN2 with anti-tumor activity and can be used to study melanoma.

Ralimetinib is a selective inhibitor that blocks phosphorylation of MK2 at Thr334, without affecting the phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib functions as an ATP-competitive inhibitor of p38 MAPK α/β, demonstrating IC50 values of 5.3 and 3.2 nM, respectively, and is under investigation as an anti-inflammatory and anticancer therapeutic.

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease and dysmenorrhoea.

Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.

Tebideutorexant is a selective antagonist of the orexin-1 receptor and has demonstrated anti-panic effects in both rodent and human models of panic-anxiety. Tebideutorexant provides valuable insights into orexin signaling pathways in stress response and has potential utility as a tool compound for psychiatric and neurobehavioral disorder research.

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

PF-610355 is a long-acting and potent β2-adrenergic receptor agonist (EC50: 0.26 nM).PF-610355 can be used to study asthma and COPD.

dWIZ-1 ((rac)-dWIZ-1) is a potent WIZ molecular gel degrader that recruits WIZ (ZF7) to the cereblon thereby inducing degradation and thus induction of haemoglobin fetalis (HbF) in erythroblasts, which can be used to study sickle cell disease (SCD).

diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a second messenger in cellular innate immunity, catalyzed by cGAMP synthase (cGAS) under DNA binding conditions. It binds to STING to form a dimer, inducing the production and expression of interferon-β and other cytokines.

ZD-6888 Hydrochloride (ZD-6888 HCl) is an angiotensin II (AII) antagonist that mediates AII receptor blockade and induces a competitive inhibition of AII-mediated renin release.

BI-4732 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with high blood-brain barrier permeability, antitumor activity, inhibition of EGFR activation, and inhibition of T790M mutations.

VAV1 degrader-2 (Example 176) is a molecular gel degrader (DC50=4.41 nM) that targets VAV 1 for the study of inflammatory and autoimmune diseases.

DNL343 is a selective and potent eIF2B activator that crosses the blood-brain barrier and inhibits the assembly of stress granules (SGs) induced by the C9ORF72 dipeptide repeats. DNL343 may be useful in the study of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS).

D-Isofloridoside, a polysaccharide precursor, exhibits free radical scavenging activity and inhibits both ROS expression and the enzymes MMP-2 and MMP-9.

FAP targeting peptide for FXX489 is the peptide component of FXX489. FXX489 is a targeting ligand that can specifically recognize and bind to fibroblast activation protein (FAP).

Cianopramine (Ro 112465) is a selective 5-hydroxytryptamine uptake inhibitor and a tricyclic antidepressant used in the study of neurological disorders.

BMS-986449 is a CELMoD-type molecular gel that remodels the function of regulatory T cells (Treg) and enhances their anti-tumor immune responses by directing the E3 ubiquitin ligase, Cereblon, to target the degradation of IKZF2 (Helios) and IKZF4 (Eos). BMS-986449 has potential application in the study of advanced solid tumors.

Thymectacin (NB 1011) is a selective thymidine synthase (TS) inhibitor with anticancer activity for the study of colon cancer and solid tumors.

PZL-A, an activator of mtDNA synthesis, restored the function and activity of the most common POLγ mutant variant and activated mtDNA synthesis in the cells of pediatric patients with fatal diseases, thereby enhancing the oxidative phosphorylation mechanism and the biogenesis of cellular respiration, and can be used to treat progressive diseases associated with mtDNA depletion.

KU-177 is a Hsp90 ATPase homolog 1 (Aha1) inhibitor. By disrupting the interaction between Hsp90 and Aha1, it prevents the proliferation of primary MM and relapsed MM patient samples. It eliminates the proliferation and PI resistance induced by AHSA1 elevation.

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor with nanomolar-level inhibitory effects on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP production, leading to impaired cellular energy metabolism and cancer cytotoxicity.

Venuloside A (ESK246), a monoprostane glycoside from Pittosporum venulosum, is a LAT3 inhibitor and a leucine uptake inhibitor that inhibits the transporter of leucine through LAT3, and may be used in the study of prostate cancer.

Eribulin (B1939) is a nonpaclitaxel microtubule kinetic inhibitor with anticancer activity that inhibits polymerization of microtubule protein subunits by preventing lengthening and shortening of microtubules during cell division.Eribulin is used in the study of metastatic breast cancer and solid tumors.

Imelciment (REGN-9035) is a humanised monoclonal antibody targeting NPR1, which can be used for research into heart failure.

DT204 is an SCFSkp2 inhibitor that reduces the binding of Skp2 to Cullin-1 and Commd1. It can be used to study multiple myeloma.

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

KRH102140 is a PHD2 activator that reduces angiogenesis by inhibiting HIF-1alpha, used in cardiovascular disease research.

RO7567132 (FAP-LTBR) is a novel bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, thereby limiting the activation of LTBR to the tumor microenvironment, inducing the formation of local tertiary lymphoid structures (TLS), and reducing systemic toxicity. Its mouse alternative can inhibit breast cancer growth, and the effect is better when combined with atezolizumab. In the mouse colorectal cancer model, it can also enhance immune cell infiltration and TLS-like structure formation.

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

MK-3984 is a selective androgen receptor modulator, used in the study of conditions caused by androgen deficiency.

QPX7728 disodium (Xeruborbactam disodium) is a cyclic boronate inhibitor of many serine and metal-β-lactamases with antibacterial activity, used in research on bacterial infections.

Suntinorexton (TAK 861) is an orexin type 2 receptor (OX2R) agonist for the study of neurological disorders.

Apelin agonist 1 is an orally available APJ receptor agonist with an EC50 value of 3.2 nM. Apelin agonist 1 is used in the study of cardiovascular disease.

Motugivatrep is a potent and selective TRPV1 antagonist that can be used to study TRPV1-related respiratory diseases.

β-Naltrexamine dihydrochloride is an orally administered, irreversible opioid receptor antagonist. Its derivatives exhibit optimised subtype selectivity and can be used for pain research.