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PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research [1].
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer [1].
PM534, tubulin targeting agent, inhibits tubulin assembly with IC50 values of 0.8-3.2 nM. PM534 binds to the colchicine site of tubulin, which has high antitumor activity .
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Ecubectedin (PM14) is a derivative. Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities .
Zalypsis (PM00104) has anti-tumor activity. Zalypsis binds to DNA and shows cytotoxicity. Zalypsis inhibits cell cycle and transcription, and leads to double stranded DNA breaks .
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo .
Plocabulin (PM060184) is a potent microtubule inhibitor. Plocabulin is a natural product that could be isolated from the marine sponge Lithoplocamia lithistoides. Plocabulin suppresses microtubule shortening and growth. Plocabulin has anticancer activity .
PM20D1 Human Pre-designed siRNA Set A contains three designed siRNAs for PM20D1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
Pyrromethene 605 (PM605) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 556 (PM556) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 650 (PM650) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Secnidazole (RP-14539) hemihydrate is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole hemihydrate, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole hemihydrate has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole hemihydrate can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
alpha-2,3-Sialyltransferase (PmST2) is a sialyltransferase produced by Pasteurella multocida (Pm) and plays an important role in the pathogenesis of Pm. alpha-2,3-Sialyltransferase (PmST2) can be used to synthesize sialyllactosyl sphingosine (lyso-GM3) .
alpha-1,3-N-Acetylgalactosaminyltransferase (Pm1138) (EC 2.4.1.40(Pm1138)), also namely the ABO system transferase with glycosyl transferase activity .
Oligomycin D (Rutamycin A) is an antibiotic. Oligomycin D can be derived from a strain of S. rutgersensis. Oligomycin D also is a potent inhibitors of K-Ras PM localization. Oligomycin D can be used for the research of various cancers .
Hongotoxin-1, isolated from venom of Centruroides limbatus, is the inhibitor of potassium channel, with IC50 for? Kv1.1, Kv1.2, Kv1.3, and Kv1.6 of 31 pM, 170 pM, 86 pM,and 6000 pM, respectively .
FC-11 is a PROTACFAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459). FC-11 degrades FAK in various cells, with DC50s of 310 pM in TM3, 80 pM in PA1, 330 pM in MDA-MB-436, 370 pM in LNCaP, and 40 pM in Ramos cells .
1-Pyrenebutanoyl-CoA is a type of coenzyme A that can non-competitively inhibit (Ki = 2 pM) phosphorylating (ADP-stimulated) respiration in rat liver mitochondria, and competitively inhibit (Ki = 2.1 pM and 15 pM) carnitine palmitoyl-CoA transferase and octanoyl-CoA transferase .
DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
DC10SMe is a DNA alkylator, can be used in the synthesis of antibody-drug conjugate (ADC). DC10SMe exhibits IC50s of 15 pM, 12 pM, and 12 pM for Ramos, Namalwa, and HL60/s cancer cells, respectively .
Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research .
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Ledipasvir diacetone (GS-5885 diacetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
IBG3 is a dual-JQ1-containing BET degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs) . Lenacapavir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM .
Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM .
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D) .
Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D) .
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
GlcNAcstatin is a selective glucoimidazole-based bacterial O-GlcNAcase inhibitor with a Ki of 4.6 pM. GlcNAcstatin shows 100000-fold selectivity over HexA/B .
Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity .
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity .
Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
ASN06917370 is a former orphan receptor GPR17 ligand for the study of neurodegenerative diseases. ASN06917370 has an EC50 of 268 pM in [35S]GTPyS experiments .
Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer .
Fluopipamine is an antagonist for Cellulose Synthase 1 (CESA1) with an IC50 of 0.78 μM. Fluopipamine leads a decrease in glucose uptake into cellulose and hyperaccumulation of CESAs at the PM in etiolated Arabidopsis seedlings .
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease .
Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro .
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
T26c sodium is a potent and selective MMP13 inhibitor with IC50 value of 6.9 pM. T26c sodium can inhibit the degradation of bovine nasal septal cartilage explants .
GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease .
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM .
Govorestat (AT-007) is an orally active brain-penetrant aldose reductase inhibitor with an IC50 value of 100 pM. Govorestat has the potential for galactose-1-phosphate uridyl transferase deficiency research .
RG7697 is a dual agonist for glucagon-like peptide receptor (GLP Receptor) and glucosedependent insulinotropic polypeptide receptor (GIPR), with EC50 of 5 and 3 pM, respectively. RG7697 exhibits antihyperglycemic property .
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP .
Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM .
Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
Ocaratuzumab (AME 133v) is an Fc-engineered humanized IgG1 anti-CD20 monoclonal antibody, with a Kd of ~100 pM. Ocaratuzumab exhibits more effective antibody-dependent cell-mediated cytotoxicity (ADCC) .
Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes .
Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.
Calmodulin Binding Peptide 1 is a high affinity (pM) CaM-binding peptide derived from smooth muscle myosin light-chain kinase (MLCK peptide), which strongly inhibits IP3-induced Ca 2+ release .
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM .
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility .
AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons .
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
Plasma kallikrein-IN-5 (Compound 20) is a potent covalent inhibitor of plasma potassium kinin peptide (Pka) with IC50 values of 66 nM and 70 pM at 1 minute and 24 hours, respectively. Plasma kallikrein-IN-5 can be used IN the study of hereditary angioedema (HAE) .
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
Ramiprilat-d5 is deuterium labeled Ramiprilat. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research[1].
Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA) .
MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
Ru-4T is a phototherapy agent. Ru-4T has phototherapeutic efficacy (PI = 114,000) against melanoma cells (SK-MEL-28) under broad-band visible light (400-700 nm) with EC50 values of 740 pM .
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis .
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM . Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells .
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
AM-7209 is a potent and selective MDM2-p53 interaction inhibitor with a Kd of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 shows antitumor activities .
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity .
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity .
DC41SMe, a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer .
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research .
SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19 .
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer .
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
Vobarilizumab (ALX-0061) is an anti-IL-6R monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis .
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease .
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER) . Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively .
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
Canakinumab (ACZ885) is a recombinant human anti-IL-1β monoclonal antibody. Canakinumab shows IC50 values of 43.6 and 40.8 pM for human and marmoset IL-1β, respectively. The mode of action of canakinumab is based on the neutralization of IL-1β signaling, resulting in suppression of inflammation related to disorders of autoimmune origin .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasma membrane (PM), causing the plasma membrane to fluoresce .
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity .
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
MRTX-1719 is a potent, orally active, selective PRMT5•MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5•MTA and PRMT5. MRTX-1719 binds to the PRMT5•MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
IMP-1088 is a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a Kd of <210 pM for HsNMT1. IMP-1088 efficiently blocks rhinovirus replication by blocking rhinovirus virus-encoded protein (VP0) N-myristoylation. IMP-1088 protects host cells from the cytotoxic effects of viral infection .
RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity .
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Bruceantinol, a quassinoid isolated from Brucea javanica, inhibits pepper mottle virus in pepper . Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50=2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
NS5A-IN-4 (Compound 1.12) is an orally active pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with IC50 values of 1.2, 2296, 4.6, 362, 10.3 and 693 pM against gT1b, gT1a, gT2a, gT3a, gT4a and gT5a . NS5A-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie [1].
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism .
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research .
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
Pyrromethene 605 (PM605) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 556 (PM556) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 650 (PM650) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasma membrane (PM), causing the plasma membrane to fluoresce .
alpha-1,3-N-Acetylgalactosaminyltransferase (Pm1138) (EC 2.4.1.40(Pm1138)), also namely the ABO system transferase with glycosyl transferase activity .
Streptavidin is a ∼60 kDa homotetramer. Streptavidin binds four molecules of biotin with the highest affinity. The binding affinity of biotin to streptavidin is one of the highest reported for a non-covalent interaction to date, with a KD ∼ 0.01 pM . Streptavidin has an immunosuppressive role .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Hongotoxin-1, isolated from venom of Centruroides limbatus, is the inhibitor of potassium channel, with IC50 for? Kv1.1, Kv1.2, Kv1.3, and Kv1.6 of 31 pM, 170 pM, 86 pM,and 6000 pM, respectively .
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D) .
Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D) .
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Nesiritide (Brain Natriuretic Peptide-32 human) is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively.
Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
RG7697 is a dual agonist for glucagon-like peptide receptor (GLP Receptor) and glucosedependent insulinotropic polypeptide receptor (GIPR), with EC50 of 5 and 3 pM, respectively. RG7697 exhibits antihyperglycemic property .
Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
Calmodulin Binding Peptide 1 is a high affinity (pM) CaM-binding peptide derived from smooth muscle myosin light-chain kinase (MLCK peptide), which strongly inhibits IP3-induced Ca 2+ release .
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-ψ-(COO)Ala-Ser-Lys(DABCYL)-NH2 (HCV NS3 protease substrate) is a biological active peptide. (This peptide is a HCV protease substrate incorporating an ester bond between residues P1 and P1. Due to ready transesterification of the scissile bond to the acyl-enzyme intermediate, this substrate shows very high kcat/Km values, enabling detection of activity with subnanomolar nonstructural protein 3 (NS3 protease) concentrations. It is widely used for the continuous assay of NS3 protease activity. Substrate cleavage is proportional to the enzyme concentration with a detection limit for NS3 between 1 nM and 250 pM. Upon cleavage of this substrate, fluorescence can be monitored at Abs/Em = 355/500 nm.)
Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research .
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
Frunevetmab (NV-02) is a felinized anti-nerve growth factor (NGF) monoclonal antibody with a Kd of 20 pM. Frunevetmab can effectively decrease osteoarthritis (OA) pain in cats .
Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer .
Narnatumab (IMC-RON8) is a neutralizing human monoclonal antibody that blocks RON binding to its ligand, macrophage-stimulating protein (MSP), with a Kd of 32 pM. Narnatumab can be used for the research of cancer .
Domagrozumab is an anti-myostatin humanized monoclonal antibody with a KD value of 2.6 pM for human myostatin. Domagrozumab induces muscle anabolic activity. Domagrozumab can be used in research of duchenne muscular dystrophy (DMD) .
Ocaratuzumab (AME 133v) is an Fc-engineered humanized IgG1 anti-CD20 monoclonal antibody, with a Kd of ~100 pM. Ocaratuzumab exhibits more effective antibody-dependent cell-mediated cytotoxicity (ADCC) .
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility .
Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA) .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
Vobarilizumab (ALX-0061) is an anti-IL-6R monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
Canakinumab (ACZ885) is a recombinant human anti-IL-1β monoclonal antibody. Canakinumab shows IC50 values of 43.6 and 40.8 pM for human and marmoset IL-1β, respectively. The mode of action of canakinumab is based on the neutralization of IL-1β signaling, resulting in suppression of inflammation related to disorders of autoimmune origin .
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism .
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research .
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
Plocabulin (PM060184) is a potent microtubule inhibitor. Plocabulin is a natural product that could be isolated from the marine sponge Lithoplocamia lithistoides. Plocabulin suppresses microtubule shortening and growth. Plocabulin has anticancer activity .
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
Bruceantinol, a quassinoid isolated from Brucea javanica, inhibits pepper mottle virus in pepper . Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50=2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc .
Galectin-1/LGALS1 is a lectin that binds β-galactoside and complex carbohydrates and regulates apoptosis, proliferation, and differentiation. It inhibits CD45 phosphatase activity, blocks Lyn kinase dephosphorylation, and induces T cell apoptosis. Animal-Free Galectin-1/LGALS1 Protein, Human (His) is the recombinant human-derived animal-FreeGalectin-1/LGALS1 protein, expressed by E. coli , with N-His labeled tag. The total length of Animal-Free Galectin-1/LGALS1 Protein, Human (His) is 134 a.a., with molecular weight of ~15.5 kDa.
Galectin-1/LGALS1 is a lectin that binds β-galactoside and complex carbohydrates and regulates apoptosis, proliferation, and differentiation. It inhibits CD45 phosphatase activity, blocks Lyn kinase dephosphorylation, and induces T cell apoptosis. Galectin-1/LGALS1 Protein, Human (His) is the recombinant human-derived Galectin-1/LGALS1 protein, expressed by E. coli , with C-6*His labeled tag. The total length of Galectin-1/LGALS1 Protein, Human (His) is 134 a.a., with molecular weight of ~15.0 kDa.
EXOSC9 is a noncatalytic RNA exosome complex component that critically drives 3'->5' exoribonuclease activity and contributes to a variety of cellular RNA processing and degradation events. In the nucleus, it helps stabilize the maturation of RNA species and eliminates processing by-products, non-coding transcripts and defective mRNAs, thereby inhibiting their cytoplasmic export. EXOSC9 Protein, Human (sf9, His) is the recombinant human-derived EXOSC9 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of EXOSC9 Protein, Human (sf9, His) is 439 a.a., with molecular weight of ~51.3 KDa.
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
Ramiprilat-d5 is deuterium labeled Ramiprilat. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research[1].
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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