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CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity .
CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity .
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia .
Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy .
Thrombospondin (TSP-1)-derived CD36 binding motif is a bioactive hexapeptide. Thrombospondin (TSP-1)-derived CD36 binding motif interferes with the interaction between cells and the extracellular matrix by binding to CD36 and angiostatin, thereby affecting the cell adhesion and migration process. Thrombospondin (TSP-1)-derived CD36 binding motif inhibits platelet aggregation. Thrombospondin (TSP-1)-derived CD36 binding motif exerts an anti-tumor effect against colon cancer .
EcAMP3 is a hairpin-like peptide. EcAMP3 has antifungal and antibacterial activity. EcAMPs precursor family contains seven identical cysteine motifs: C1XXXC2(11–13)C3XXXC4 .
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif .
μ-TRTX-Hd1a, a spider venom, is a selective NaV 1.7 inhibitor. μ-TRTX-Hd1a is a gating modifier that inhibits human NaV 1.7 by interacting with the S3b-S4 paddle motif in channel domain II .
N3-Gly-Gly-Gly-OH is a oligo-Gly click chemistry reagent containing an azide group. Oligo-Gly also has been used as linker to combine different subunits of dimeric or oligomeric proteins or to create artificial multi-domain proteins. By modification into Gly-Gly-Gly-Ser motifs high solubility can be achieved . N3-Gly-Gly-Gly-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia .
Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
Adamtsostatin 18 is an anti-angiogenic peptide derived from proteins containing type I thrombospondin motifs. Adamtsostatin 18 inhibits cell migration and proliferation .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
FlAsH-EDT2 is a protein labeling reagent. FlAsH-EDT2 binds to Cys4 with high affinity and emits fluorescence. FlAsH-EDT2 can cross the cell membrane and enter the interior of the cell. FlAsH-EDT2 can only be used for labeling proteins with high concentration .
Protein O-Fucosyltransferase 1 (EC:2.4.1.221; POFUT1) is a Glycosyltransferase containing the cysteine-rich motifs as the acceptor sugar and GDP-fucose as the donor .
ORN 02 is a synthetic single-stranded U-rich RNA and contains 6 repeats of UUAU sequence motif. The AU-rich oligoribonucleotides (ORNs) are able to stimulate TLR8 .
ORN 02 (sodium) is a synthetic single-stranded U-rich RNA and contains 6 repeats of UUAU sequence motif. The AU-rich oligoribonucleotides (ORNs) are able to stimulate TLR8 .
Gap 26 is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif .
ORN 06 (sodium) s a synthetic single-stranded U-rich RNA and contains 6 repeats of the UUGU sequence motif. The GU-rich oligoribonucleotides (ORNs) are able to stimulate TLR7 .
Fmoc-Cit-OH (Fmoc-L-Citrulline) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize a degradable ADC linker composed of a valine-citrulline (Val-Cit) motif .
Gap 26 TFA is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif .
ODN 5328 (ODN 2395 Control) can be used as a sequence control for C-class ODN 2395. ODN 5328 shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
ODN 5328 (ODN 2395 Control) sodium can be used as a sequence control for C-class ODN 2395. ODN 5328 sodium shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
Sp-TTPαS is a competitivesterile alpha motif and HD domain containing protein 1 (SAMHD1) catalysis inhibitor. Sp-TTPαS competitively inhibits TTP hydrolysis with a Ki value of 46 µM .
Teixobactin is a potent antibiotic. Teixobactin shows antibacterial activity for gram-negative bacteria. Teixobactin inhibits cell wall synthesis by binding to a highly conserved motif of lipid II and lipid III .
NGR peptide Trifluoroacetatecontaining the Asn-Gly-Arg (NGR) motif. NGR peptide Trifluoroacetate binds to APN/CD13. NGR peptide Trifluoroacetate is directly conjugated to imaging agents that can be used for tumor imaging .
NGR peptide containing the Asn-Gly-Arg (NGR) motif. NGR peptide binds to APN/CD13. NGR peptide is directly conjugated to imaging agents that can be used for tumor imaging .
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
9(R)-HODE is a monohydroxy fatty acid and metabolite of linoleic acid. It is formed from linoleic acid by COX and lipoxygenase (LO).9(R)-HODE induces chemotaxis, increases the levels of chemokine (C-C motif) receptor 9 (CCR9) and chemokine (C-X-C motif) receptor 4 (CXCR4), and inhibits IL-6 release in primary human monocytes. It inhibits CD3α- and CD28-induced proliferation of isolated human peripheral blood lymphocytes when used at a concentration of 25 μg/mL.
LSTc (LS-tetrasaccharide c) is a human lactooligosaccharide presents on glycoproteins and glycolipids. LSTc is also a specific human JC polyomavirus (JCV) recognition motif. LSTc has good potential for the study of progressive multifocal leukoencephalopathy (PML) .
Enzelkitug is a humanized immunoglobulin G1-κ monoclonal antibody targeting the human C-C motif chemokine receptor 8 (CCR8). Enzelkitug is promising for research of various solid tumors and hematological malignancies .
ODN 1982 is a unmethylated oligodeoxyribonucleotide (ODN) with no CpG motif, can be used to prepare DNA vaccines. ODN 1982 inhibits R-848 signaling. ODN 1982 sequence: 5’-tccaggacttctctcaggtt-3’ .
ICMT-IN-21 (compound 6ag) is an ICMT inhibitor (IC50=8.8 μM), a sulfonamide-modified farnesyl cysteine (SMFC). The farnesyl and carboxylic acid motifs of ICMT-IN-21 are important structures for inhibiting ICMT .
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
3X FLAG peptides are FLAG-tagged peptides containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide can be used for protein separation and purification, and competitive elution with target proteins.
Histone H1-derived Peptide is a phosphopeptide and the peptide substrates containes a sequence in accordance with the optimal recognition motif for CDK, can be used to detecting CDK1-cyclinB1 enzyme activity .
Harmalol is a β-carbazine alkaloid with anticancer activity. Harmalol binds and interacts with several natural and synthetic nucleic acids of different motifs, including DNA and RNA. In addition, harmalol has an apoptosis-inducing effect on human hepatoma cells in vitro .
ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif .
Azide-PEG8-Tos is a small PEG linker featuring an azide and a tosylate. Tosylates are good leaving groups which are easily displaced by nucleophiles while azide is a click chemistry motif which is used to react with terminal alkynes or strained cyclooctynes.
TAT-CBD3, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization .
DNP-PEG2-NHCO-C2-DBCO is a clickable hapten that bears a dinitrophenyl (DNP) moiety as the antibody‐recruiting motif at one end, a polyethylene glycol chain as a spacer and a dibenzocyclooctene at the other end for the SPAAC chemistry .
L-739750 is a selective protein farnesyltransferase (PFTase) inhibitor (IC50: 0.4 nM). PFTase utilizes farnesyl diphosphate to farnesylate the cysteine residue of protein substrates having a C-terminal CAAX motif. L-739750 is a selective CAAX peptidomimetic .
NH2-MPAA-NODA is a nitroveratryl-based photocleavable linker, it has a NODA motif and a methyl phenyl acetic acid (MPAA) backbone . NH2-MPAA-NODA can be used as a radiolabel by labeling with 18F-fluoride.
JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation .
CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation .
ssVACV-70mer sodium is a 70 bp single-stranded oligonucleotide containing viral DNA motifs that derive from the vaccinia virus DNA. Unlike its double-stranded counterpart dsVACV 70mer, ssVACV 70mer is not IFN-inducer .
beta-1,4-Galactosyltransferase 1 (Y285L) can enzymatic synthesis of the LacdiNAc motif. beta-1,4-Galactosyltransferase 1 (Y285L) can transfer of GalNAc from UDP-GalNAc .
WIZ degrader 1 (Compound 141) is a degrader for widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. WIZ degrader 1 induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM. WIZ degrader 1 is used in research of inherited blood disorders .
dsVACV-70mer sodium is a 70 bp double-stranded oligonucleotide containing viral DNA motifs derived from vaccinia virus DNA. dsVACV-70mer sodium has potently induces IFN-β via a STING-dependent manner .
BMP2-derived peptide is a functional motif from positions 73 to 92 of the amino acid sequence of BMP-2. BMP2-derived peptide promotes osteogenic differentiation of bone marrow stromal cells (BMSCs) and enhances bone regeneration .
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs) .
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1 .
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 corresponding to amino acids 148-156 of the BRLF1 protein. BRLF1 is a transcriptional activator that binds directly to a GC-rich motif present in some Epstein-Barr virus (EBV) lytic gene promoters .
2-Methoxyhydroquinone is a phenolic compound that reduces TNF-α-induced production of chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 64.3 µM. 2-Methoxyhydroquinone is also a precursor in the synthesis of the Hsp90 inhibitor Geldanamycin (HY-15230) .
WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders .
CTT2274 is a prodrug of MMAE (HY-15162). CTT2274 is composed of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and MMAE payload. CTT2274 shows selective binding to PSMA and delivers MMAE. CTT2274 inhibits prostate cancer .
Grb2 SH2 domain inhibitor 1 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration .
Emapticap pegol sodium is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol sodium is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
ORN 06 (Compound R-0006), a U-rich single-stranded RNA (containing 6 repeats of the UUG sequence motif), is a TLR7/8 agonist. ORN 06 stimulates human TLR7/8-mediated or murine TLR7-mediated immunity .
SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing .
Grb2 SH2 domain inhibitor 1 TFA is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
Ianalumab (VAY-736) is a human, decarboxylated antibody against BAFF-R. Ianalumab can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF. Ianalumab exerts antibody-dependent cytotoxic (ADCC), depending on effector cell activation mediated by immune receptor tyrosine activation motif (ITAM) .
ANK peptide is a novel peptide designed based on the conserved residues of single ankyrin motif. ANK peptide is a synuclein-γ (SNCG) inhibitor that binds to SNCG and competes with SNCG-BubR1 interaction to enhance the sensitivity of breast cancer cells to antimicrotubule drugs such as nocodazole and paclitaxel. ANK peptide can be used in the study of cancer .
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus .
WIZ degrader 3 (Compound 29) is a degrader for widely interspaced zinc finger motifs (WIZ), with an AC50 of 6.4 nM. WIZ degrader 3 induces the expression of fetal hemoglobin (HbF), with an EC50 of 45 nM. WIZ degrader 3 can be used for the research of blood disorders, such as sickle cell disease and β- thalassemia .
UHMCP1 is a chemical probe of U2AF homology motifs (UHM) with a Kd of 79 μM. UHMCP1 prevents the SF3b155/U2AF65 interaction, impacts RNA splicing and cell viability. UHMCP1 has potential anticancer properties .
Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases .
CMV pp65(13-27) is a biological active peptide. (This peptide is derived from amino acid residues 13 to 27 of the 65k lower matrix phosphoprotein of the human cytomegalovirus. It contains a nine-amino-acid sequence (LGPISGHVL) that matches the consensus binding motif for a major histocompatibility complex H2-Dd T-cell epitope.)
L-739758 is an antagonist for αIIbβ3 integrin (platelet glycoprotein IIb/IIIa). L-739758 acts as a peptidomimetic, binds to αIIbβ3 integrin by mimicking the interaction of the RGD (arginine-glycine-aspartic acid) motif, and is involved in the blood coagulation process. L-739758 inhibits platelet aggregation, and is used for thrombosis research .
DBCO-PEG2-Val-Cit-PAB-MMAE is an ADC linker featuring a DBCO group, a Val-Cit dipeptide, a PAB motif, and an MMAE warhead. The DBCO group is a click chemistry handle which readily reacts with azide groups, while the Val-Cit is a protease-cleavable dipeptide which releases the MMAE warhead into cells via an elimination mechanism.
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
244cis, a piperazine-containing ionizable cationic lipid, has been used to generate lipid nanoparticles (LNPs). LNPs containing 244cis and coated with mRNA reporter gene were specifically accumulated in mouse lungs compared with LNPs containing SM-102. Induces a decrease in serum chemokine (C-C motif) ligand 2 (CCL2) levels .
Cathepsin E substrate e is a substrate of Cathepsin E. Cathepsin E substrate e was designed in such a way that due to the close proximity of a Mca-donor and a Dnp-acceptor, a near complete intramolecular quenching effect was achieved in its intact state. After the proteolytic cleavage of the hydrophobic motif of the peptide substrate, both Mca and Dnp would be further apart, resulting in bright fluorescence .
AP39 (Item No. 17100) is a compound used to increase the levels of hydrogen sulfide (H2S) within mitochondria. It consists of a mitochondria-targeting motif (triphenylphosphonium) coupled to an H2S-donating moiety (dithiolethione) by an aliphatic linker. AP219 is a control compound for AP39, containing the triphenylphosphonium scaffold but lacking the H2S-releasing portion.
PTBP1-RNA-binding inhibitor P6 (PTBP1 α3-helix derived peptide P6) TFA is a stapled peptide inhibitor of the splicing factor PTBP1, which inhibits alternative splicing events regulated by PTBP1. PTBP1 binds RNA through its RNA recognition motif .
γ-2-MSH (41-58), amide is derived from γ-2-MSH. γ-2-MSH is a twelve amino acid peptide that is derived from the N-terminal fragment of proopiomelanocortin (POMC) and contains the His-Phe-Arg-Trp motif common to all melanocortin endogenous agonist ligands .
rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex .
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R), a chimeric peptide consisting of 29 amino acids, is synthesized by adding nona-arginine motif to the carboxy terminus of RVG (rabies virus glycoprotein). Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) is positively charged and able to bind negatively charged nucleic acids via charge interaction .
mgc(3Me)FDA is fluorescein diacetate (FDA) modified with a cell-permeable myrGC 3Memotif. mgc(3Me)FDA can enter cells and be converted into fluorescently active mgc(3Me)FL (HY-D2301) within the cells. mgc(3Me)FDA is subcellularly localized in the Golgi apparatus and is a visualized Golgi probe .
Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders .
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the research of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220) .
NSCLC-IN-1 (Compound A10-2) induces mitophagy and ferroptosis through targeting transmembrane BAX inhibitor motif containing 6 (TMBIM6). NSCLC-IN-1 induces mitochondrial Ca 2+ imbalance, leading to mitochondrial damage. NSCLC-IN-1 reduces intracellular glutathione (GSH), increases the accumulation of lipid peroxides (LPO) and malondialdehyde (MDA) content. NSCLC-IN-1 is a potent anti-NSCLC agent .
BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM .
EP39 is a potent HIV-1 maturation inhibitor. EP39 interacts with the SP1 domain of Gag. EP39 decreases the dynamics of CA-SP1 junction, by binding to the QVT motif of the SP1 domain, and perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure. EP39 acts by arresting maturation of HIV-1 thereby blocking its infectivity .
WAAG-3R TFA is a biological active peptide. (Aggrecanases belong to the ADAMTS (A disintegrin and metalloprotease with thrombospondin motif) family of proteases. Aggrecanases cleave aggrecan, the major structural component of cartilage. Aggrecanase-1 (ADAMTS-4) is a major aggrecanase in human osteoarthritic cartilage. This FRET peptide was used in an ADAMTS-4 (Aggrecanase-1) and ADAMTS-5 (Aggrecanase-2) assay . (Ex/Em = 340/420 nm)
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth .
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEADmotifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex . Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM) . Zotatifin induces cell apoptosis .
Methyl 3,4-dibromo-2,5-dioxo-2,5-dihydro-1H-pyrrole-1-carboxylate is a small pyrrolidone molecule which features two bromine atoms and a methyl ester. The unsaturated dibromo motif is a covalent ligand for thiol groups, and may be used to label cysteine residues in proteins. The presence of two leaving groups on this molecule allows this linker to bind two thiols at a time. The methyl ester can be saponified to link this molecule to amines to form larger structures.
Resolvin D2 n-3 DPA is a specialized proresolving mediator (SPM). Resolvin D2 n-3 DPA (1 nM) can reduce the chemotaxis and adhesion of human neutrophils induced by TNF-α. Resolvin D2 n-3 DPA (100 ng/mouse; intravenous injection) can reduce neutrophil infiltration in the peritoneum and the levels of IL-6 and the chemokine (C-C motif) ligand 2 (CCL2) in a mouse model of inflammation induced by zinc oxide .
HSV-60mer sodium is a 60 bp double-stranded oligonucleotide containing viral DNA motifs that derive from the herpes simplex virus 1 (HSV-1) genome . Transfected HSV-60 has been shown to potently induce IFN-β in a Toll-like receptor (TLR)-, DNA-dependent activator of IRFs (DAI)-, and RNA polymerase III (Pol III)-independent, but STING-, TBK1- and IFN regulatory factor 3 (IRF3)-dependent manner.
Tyrosinase-related Protein 2 (TRP-2) (181-188) is a tyrosinase-related protein 2 (TRP-2)-derived peptide, corresponding to residues 180-188. Tyrosinase-related Protein 2 (TRP-2) (181-188) is the major reactive epitope within TRP-2 recognized by anti-B16 CTLs. Tyrosinase-related Protein 2 (TRP-2) (181-188) is a peptide conforming to the MHC class I H2-Kb binding motif .
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism .
NSC 194308, a U2AF2-RNA complexes enhancer, increases association of the U2AF1-U2AF2-SF1-splice site RNA complex by binding a site between the U2AF2 RNA recognition motifs (RRM1 and RRM2). NSC 194308 inhibits pre-mRNA splicing by stalling spliceosome assembly at the point where U2AF helps recruit U2 snRNP to the branchpoint. NSC 194308 enhances the binding of pre-mRNA to U2AF2, selectively triggering cell death in leukemia cell lines containing spliceosome mutations .
BP Fluor 430 Picolyl Azide is an advanced fluorescent probe that incorporatess a copper-chelating motif to raise the effective concentration of Cu(I) at the reaction site. The rate of the CuAAC reaction depends on the concentrations of all reagents, including copper, therefore raising the effective copper concentration at the reaction site will dramatically increase the rate of CuAAC reaction without the need to increase concentration of azide reagent or copper.
In addition, the use of BP Fluor 430 Picolyl Azide instead of conventional BP Fluor 430 Azide allows for at least a tenfold reduction in the concentration of the copper catalyst without sacrificing the efficiency of labeling.
In summary, the introduction of a picolyl moiety into an azide probe leads to a substantial increase in the sensitivity of alkyne detection. This is of special value for the detection of low abundance targets or where significant increase in signal intensity is desired.
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
BP Fluor 405 Picolyl Azide is an advanced fluorescent probe that incorporatess a copper-chelating motif to raise the effective concentration of Cu(I) at the reaction site. The rate of the CuAAC reaction depends on the concentrations of all reagents, including copper, therefore raising the effective copper concentration at the reaction site dramatically increases the rate of CuAAC reaction without increasing the concentrations of azide reagent or copper.
In addition, the use of picolyl azide instead of conventional azides allows for at least a tenfold reduction in the concentration of the copper catalyst without sacrificing the efficiency of labeling.
In summary, the introduction of a picolyl moiety into an azide probe leads to a substantial increase in the sensitivity of alkyne detection. This is of special value for the detection of low abundance targets or where significant increase in signal intensity is desired.
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
LC-04-045 is a NEK7 (NIMA-related kinase 7) molecular glue degrader (MGD). LC-04-045 demonstrates potent activity of NEK7 degradation with a DC50 (half-maximal degradation) of 7 nM and a Dmax (maximum degradation) of 90% in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome. LC-04-045 degrades NEK7 mediated by the ubiquitin-proteasome system (UPS) and relies on the glycine 57 (G57)-containing degron motif in NEK7. LC-04-045 effectively inhibits secretion of IL-1β and IL-18 with IC50s of 33.03 nM and 32.99 nM, respectively. LC-04-045 is potential for inflammatory diseases research .
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
With MCE's 40,662 BBs, covering around 273 reaction types, more than 40 million molecules were generated. Compounds which comply with Ro5 criteria were selected. Inappropriate chemical structures, such as PAINS motifs and synthetically difficult accessible, were removed. Based on Morgan Fingerprint, molecular clustering analysis was carried out, and molecules close to each clustering center were extracted to form this drug-like and synthesizable diversity library. These selected molecules have 805,822 unique Bemis-Murcko Scaffolds (BMS) with diversified chemical space. This library is highly recommended for AI-based lead discovery, ultra-large virtual screening and novel lead discovery.
A diversity compound library contains 1,000,000 compounds with drug fragments. Each compound has at least one drug fragment. These selected molecules have 702,902 Bemis-Murcko Scaffolds (BMS) with drug-like chemical space. This library is highly recommended for AI-based lead discovery, ultra-large virtual screening and novel lead discovery.
A Lead-like, diverse library is the foundation for achieving biological activity diversity. The MCE Lead-like Diverse Library Plus is a further supplement to the 50K Lead-like Compound Library (HY-L901), consisting of over 80,000 lead-like compounds, with an additional 30,000 structurally novel lead-like molecules. These compounds occupy a broader "chemical space", making it a powerful tool for new drug discovery.
Fragment-based drug discovery (FBDD) is well suited for discovering both drug leads and chemical probes of protein function. 3-dimensionality (3D) diversity is pivotal because the molecular shape is one of the most important factors in molecular recognition by a biomolecule. There is a developing appreciation that 3D fragments could offer opportunities that are not provided by 2D fragments.
MCE 3D Diverse Fragment Library consists of 5,400 non-flat fragment-like molecules (average Fsp3 value 0.58). More than 4,700 fragment compounds contain at least one chiral center in the structure. The key concepts that underlie the library design were 3D shape, structural diversity, reactive functionality and fragment-like. This 3D Diverse Fragment Library brings higher fragment hit optimization and increases the likelihood to find innovative hits in FBDD.
On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.
The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.
MCE 5K Scaffold Library consists of 5,000 lead-like compounds. Each compound represents one unique scaffold. All compounds are compatible with Lipinski’s rule (Rule of 5) with multiple characteristics such as calculated good solubility (-3.2 < logP < 5), oral bioavailability (RotB <= 10), drug transportability (PSA < 120). Compounds contained within the library have been screened to remove any inappropriate chemical structures, avoiding “false hits”. The sufficient diverse of compound structure makes this library a powerful tool for drug screening.
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 5K Natural Product-like Compound Library consists of 5,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
MegaUni 50K Virtual Diversity Library consists of 50,000 novel, synthetically accessible, lead-like compounds. With MCE's 40,662 Building Blocks, covering around 273 reaction types, more than 40 million molecules were generated. Based on Morgan Fingerprint and Tanimoto Coefficient, molecular clustering analysis was carried out, and molecules closest to each clustering center were extracted to form a drug-like and synthesizable diversity library. The selected 50,000 drug-like molecules have 46,744 unique Bemis-Murcko Scaffolds (BMS), each containing only 1-3 compounds. This diverse library is highly recommended for virtual screening and novel lead discovery.
MCE 50K Diversity Library consists of 50,000 lead-like compounds with multiple characteristics such as calculated good solubility (-3.2 < logP < 5), oral bioavailability (RotB <= 10), drug transportability (PSA < 120). These compounds were selected by dissimilarity search with an average Tanimoto Coefficient of 0.52. There are 36,857 unique scaffolds and each scaffold 1 to 7 compounds. What’s more, compounds with the same scaffold have as many functional groups as possible, which make abundant chemical spaces. This exceptionally diverse library is highly recommended for random screening against new as well as popular targets based its novel, diverse scaffolds, abundant chemical spaces and the convenience for subsequent modification.
mgc(3Me)FDA is fluorescein diacetate (FDA) modified with a cell-permeable myrGC 3Memotif. mgc(3Me)FDA can enter cells and be converted into fluorescently active mgc(3Me)FL (HY-D2301) within the cells. mgc(3Me)FDA is subcellularly localized in the Golgi apparatus and is a visualized Golgi probe .
BP Fluor 430 Picolyl Azide is an advanced fluorescent probe that incorporatess a copper-chelating motif to raise the effective concentration of Cu(I) at the reaction site. The rate of the CuAAC reaction depends on the concentrations of all reagents, including copper, therefore raising the effective copper concentration at the reaction site will dramatically increase the rate of CuAAC reaction without the need to increase concentration of azide reagent or copper.
In addition, the use of BP Fluor 430 Picolyl Azide instead of conventional BP Fluor 430 Azide allows for at least a tenfold reduction in the concentration of the copper catalyst without sacrificing the efficiency of labeling.
In summary, the introduction of a picolyl moiety into an azide probe leads to a substantial increase in the sensitivity of alkyne detection. This is of special value for the detection of low abundance targets or where significant increase in signal intensity is desired.
BP Fluor 405 Picolyl Azide is an advanced fluorescent probe that incorporatess a copper-chelating motif to raise the effective concentration of Cu(I) at the reaction site. The rate of the CuAAC reaction depends on the concentrations of all reagents, including copper, therefore raising the effective copper concentration at the reaction site dramatically increases the rate of CuAAC reaction without increasing the concentrations of azide reagent or copper.
In addition, the use of picolyl azide instead of conventional azides allows for at least a tenfold reduction in the concentration of the copper catalyst without sacrificing the efficiency of labeling.
In summary, the introduction of a picolyl moiety into an azide probe leads to a substantial increase in the sensitivity of alkyne detection. This is of special value for the detection of low abundance targets or where significant increase in signal intensity is desired.
Protein O-Fucosyltransferase 1 (EC:2.4.1.221; POFUT1) is a Glycosyltransferase containing the cysteine-rich motifs as the acceptor sugar and GDP-fucose as the donor .
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia .
Thrombospondin (TSP-1)-derived CD36 binding motif is a bioactive hexapeptide. Thrombospondin (TSP-1)-derived CD36 binding motif interferes with the interaction between cells and the extracellular matrix by binding to CD36 and angiostatin, thereby affecting the cell adhesion and migration process. Thrombospondin (TSP-1)-derived CD36 binding motif inhibits platelet aggregation. Thrombospondin (TSP-1)-derived CD36 binding motif exerts an anti-tumor effect against colon cancer .
EcAMP3 is a hairpin-like peptide. EcAMP3 has antifungal and antibacterial activity. EcAMPs precursor family contains seven identical cysteine motifs: C1XXXC2(11–13)C3XXXC4 .
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif .
μ-TRTX-Hd1a, a spider venom, is a selective NaV 1.7 inhibitor. μ-TRTX-Hd1a is a gating modifier that inhibits human NaV 1.7 by interacting with the S3b-S4 paddle motif in channel domain II .
CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia .
ALPS1 peptide from ArfGAP1 is a curvature selective peptide from ArfGAP1 ALPS1 motif. Curvature selectivity can be used to develop broad-spectrum antiviral peptides .
Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
Adamtsostatin 18 is an anti-angiogenic peptide derived from proteins containing type I thrombospondin motifs. Adamtsostatin 18 inhibits cell migration and proliferation .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
Arg-Gly-Asp-Cys TFA is the binding motif of fibronectin to cell adhesion molecules. Arg-Gly-Asp-Cys TFA can inhibit platelet aggregation and fibrinogen binding .
Gap 26 is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif .
Pheromone Biosynthesis Activating Neuropeptide (Helicoverpa assulta, Heliothis zea) (PBAN), a member of the PBAN/Pyrokinin neuropeptide family, characterized by a common amino acid sequence FXPRLamide motif in the C-terminus .
Fmoc-Cit-OH (Fmoc-L-Citrulline) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize a degradable ADC linker composed of a valine-citrulline (Val-Cit) motif .
Gap 26 TFA is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif .
VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
Teixobactin is a potent antibiotic. Teixobactin shows antibacterial activity for gram-negative bacteria. Teixobactin inhibits cell wall synthesis by binding to a highly conserved motif of lipid II and lipid III .
Tetraproline is a fragment sequence in tristetraprolin (TTP). Recruitment of the 4EHP-GYF2 cap-binding complex to tetraproline motifs of tristetraprolin promotes repression and degradation of mRNAs with AU-rich elements .
NGR peptide Trifluoroacetatecontaining the Asn-Gly-Arg (NGR) motif. NGR peptide Trifluoroacetate binds to APN/CD13. NGR peptide Trifluoroacetate is directly conjugated to imaging agents that can be used for tumor imaging .
NGR peptide containing the Asn-Gly-Arg (NGR) motif. NGR peptide binds to APN/CD13. NGR peptide is directly conjugated to imaging agents that can be used for tumor imaging .
BRC4wt (BRC4 repeat motif) is part of the BRACA2 tumor suppressor protein, which exhibits inhibitory activity against interaction of the BRACA2 protein with RAD51, and is involved in the repair of DNA damage .
3X FLAG peptides are FLAG-tagged peptides containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide can be used for protein separation and purification, and competitive elution with target proteins.
Histone H1-derived Peptide is a phosphopeptide and the peptide substrates containes a sequence in accordance with the optimal recognition motif for CDK, can be used to detecting CDK1-cyclinB1 enzyme activity .
TAT-CBD3, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization .
3X FLAG peptide TFA is a FLAG-tagged peptide containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide TFA can be used for protein separation and purification, and competitive elution with target proteins.
IRS1-derived peptide is a biological active peptide. (This is a peptide fragment (979-989) of the insulin receptor substrate-1 containing the sequence motif YMXM known to bind to the two domains of SH2 on the 85kDa subunit of phosphoinositide 3-kinase.)
BMP2-derived peptide is a functional motif from positions 73 to 92 of the amino acid sequence of BMP-2. BMP2-derived peptide promotes osteogenic differentiation of bone marrow stromal cells (BMSCs) and enhances bone regeneration .
Ala-Gly-Ala is a prototype of a general tripeptide Xxx-Gly-Zzz. Except glycine and proline, there can be 18 possible amino acids for Xxx and another 18 amino acids for Zzz. Ala-Gly-Ala can be used as a model for up to 324 possible motifs of this kind of tripeptide .
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 corresponding to amino acids 148-156 of the BRLF1 protein. BRLF1 is a transcriptional activator that binds directly to a GC-rich motif present in some Epstein-Barr virus (EBV) lytic gene promoters .
Grb2 SH2 domain inhibitor 1 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
Grb2 SH2 domain inhibitor 1 TFA is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
ANK peptide is a novel peptide designed based on the conserved residues of single ankyrin motif. ANK peptide is a synuclein-γ (SNCG) inhibitor that binds to SNCG and competes with SNCG-BubR1 interaction to enhance the sensitivity of breast cancer cells to antimicrotubule drugs such as nocodazole and paclitaxel. ANK peptide can be used in the study of cancer .
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus .
Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases .
CMV pp65(13-27) is a biological active peptide. (This peptide is derived from amino acid residues 13 to 27 of the 65k lower matrix phosphoprotein of the human cytomegalovirus. It contains a nine-amino-acid sequence (LGPISGHVL) that matches the consensus binding motif for a major histocompatibility complex H2-Dd T-cell epitope.)
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
Cathepsin E substrate e is a substrate of Cathepsin E. Cathepsin E substrate e was designed in such a way that due to the close proximity of a Mca-donor and a Dnp-acceptor, a near complete intramolecular quenching effect was achieved in its intact state. After the proteolytic cleavage of the hydrophobic motif of the peptide substrate, both Mca and Dnp would be further apart, resulting in bright fluorescence .
PTBP1-RNA-binding inhibitor P6 (PTBP1 α3-helix derived peptide P6) TFA is a stapled peptide inhibitor of the splicing factor PTBP1, which inhibits alternative splicing events regulated by PTBP1. PTBP1 binds RNA through its RNA recognition motif .
γ-2-MSH (41-58), amide is derived from γ-2-MSH. γ-2-MSH is a twelve amino acid peptide that is derived from the N-terminal fragment of proopiomelanocortin (POMC) and contains the His-Phe-Arg-Trp motif common to all melanocortin endogenous agonist ligands .
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R), a chimeric peptide consisting of 29 amino acids, is synthesized by adding nona-arginine motif to the carboxy terminus of RVG (rabies virus glycoprotein). Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) is positively charged and able to bind negatively charged nucleic acids via charge interaction .
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
WAAG-3R is a biological active peptide. (Aggrecanases belong to the ADAMTS (A disintegrin and metalloprotease with thrombospondin motif) family of proteases. Aggrecanases cleave aggrecan, the major structural component of cartilage. Aggrecanase-1 (ADAMTS-4) is a major aggrecanase in human osteoarthritic cartilage. This FRET peptide was used in an ADAMTS-4 (Aggrecanase-1) and ADAMTS-5 (Aggrecanase-2) assay . (Ex/Em = 340/420 nm)
Dby HY Peptide (608-622), mouse is a biological active peptide. (Dby HY Peptide, NAGFNSNRANSSRSS, is a HYAb epitope belonging to a well-conserved family of genes coding for known or putative RNA helicases and containing a core sequence with a DEAD (Asp-Glu-Ala-Asp) box peptide motif, hence the name Dby (Dead box RNA helicase Y). The single Phenylalanine in the sequence serves as the anchor point while FNSNRANSS most likely is the “core” sequence of this HYAb epitope.)
WAAG-3R TFA is a biological active peptide. (Aggrecanases belong to the ADAMTS (A disintegrin and metalloprotease with thrombospondin motif) family of proteases. Aggrecanases cleave aggrecan, the major structural component of cartilage. Aggrecanase-1 (ADAMTS-4) is a major aggrecanase in human osteoarthritic cartilage. This FRET peptide was used in an ADAMTS-4 (Aggrecanase-1) and ADAMTS-5 (Aggrecanase-2) assay . (Ex/Em = 340/420 nm)
DABCYL-LPETG-EDANS is a biological active peptide. (This 5-amino acid peptide is a sortase substrate, C-terminal sorting signal. Sortase cleaves surface proteins at the LPXTG motif and catalyzes the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Sortases are a family of Gram-positive transpeptidases responsible for anchoring surface protein virulence factors to the peptidoglycan cell wall layer. Cleavage of this FRET substrate by sortase reveals the fluorescent signal, Abs/Em = 340/490 nm.)
Tyrosinase-related Protein 2 (TRP-2) (181-188) is a tyrosinase-related protein 2 (TRP-2)-derived peptide, corresponding to residues 180-188. Tyrosinase-related Protein 2 (TRP-2) (181-188) is the major reactive epitope within TRP-2 recognized by anti-B16 CTLs. Tyrosinase-related Protein 2 (TRP-2) (181-188) is a peptide conforming to the MHC class I H2-Kb binding motif .
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism .
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
Ianalumab (VAY-736) is a human, decarboxylated antibody against BAFF-R. Ianalumab can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF. Ianalumab exerts antibody-dependent cytotoxic (ADCC), depending on effector cell activation mediated by immune receptor tyrosine activation motif (ITAM) .
Enzelkitug is a humanized immunoglobulin G1-κ monoclonal antibody targeting the human C-C motif chemokine receptor 8 (CCR8). Enzelkitug is promising for research of various solid tumors and hematological malignancies .
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
LSTc (LS-tetrasaccharide c) is a human lactooligosaccharide presents on glycoproteins and glycolipids. LSTc is also a specific human JC polyomavirus (JCV) recognition motif. LSTc has good potential for the study of progressive multifocal leukoencephalopathy (PML) .
Harmalol is a β-carbazine alkaloid with anticancer activity. Harmalol binds and interacts with several natural and synthetic nucleic acids of different motifs, including DNA and RNA. In addition, harmalol has an apoptosis-inducing effect on human hepatoma cells in vitro .
The ADAMTS13 protein, a metalloproteinase, has a metalloproteinase domain, a disintegrin-like domain, and a thrombospondin type 1 motif. It cleaves von Willebrand Factor and defects in this gene cause thrombotic thrombocytopenic purpura. Alternative splicing generates multiple transcript variants. ADAMTS13 is broadly expressed in various tissues, including the liver, testis, and 24 other tissues. ADAMTS13 Protein, Human (CHO, His) is the recombinant human-derived ADAMTS13, expressed by CHO , with C-10*His labeled tag.
SIRP alpha/CD172a Protein, Human (CAA71403.1, HEK 293, His)
, as a recombinant protein produced in HEK293 cells, is a polypeptide chain with a His tag.
A disintegrin and metalloproteinase with thrombospondin motifs 5; A disintegrin like and metalloprotease (reprolysin type) with thrombospondin type 1 motif 5; A Disintigrin And Metalloproteinase with ThromboSpondin motif-5; ADAM metallopeptidase with thrombospondin type 1 motif 5; ADAM TS 11; ADAM TS 5; ADAM TS5; ADAMTS 11; ADAMTS 5; ADAMTS11; ADMP 2; ADMP2; Aggrecanase 2; aggrecanase-2; FLJ36738; Implantin; ThromboSpondin motif-5.
WB, ICC/IF, FC
Human, Mouse, Rat
ADAMTS5 Antibody is an unconjugated, approximately 102 kDa, rabbit-derived, anti-ADAMTS5 monoclonal antibody. ADAMTS5 Antibody can be used for: WB, IF-Cell, FC expriments in human, mouse, rat background without labeling.
SIRPA; BIT; MFR; MYD1; PTPNS1; SHPS1; SIRP; Tyrosine-protein phosphatase non-receptor type substrate 1; SHP substrate 1; SHPS-1; Brain Ig-like molecule with tyrosine-based activation motifs; Bit; CD172 antigen-like family member A; Inhibito
WB, FC
Human
SIRP alpha Antibody (YA1361) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1361), targeting SIRP alpha. SIRP alpha Antibody (YA1361) can be used for FC,WB experiment in human background.
N3-Gly-Gly-Gly-OH is a oligo-Gly click chemistry reagent containing an azide group. Oligo-Gly also has been used as linker to combine different subunits of dimeric or oligomeric proteins or to create artificial multi-domain proteins. By modification into Gly-Gly-Gly-Ser motifs high solubility can be achieved . N3-Gly-Gly-Gly-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
DNP-PEG2-NHCO-C2-DBCO is a clickable hapten that bears a dinitrophenyl (DNP) moiety as the antibody‐recruiting motif at one end, a polyethylene glycol chain as a spacer and a dibenzocyclooctene at the other end for the SPAAC chemistry .
DBCO-PEG2-Val-Cit-PAB-MMAE is an ADC linker featuring a DBCO group, a Val-Cit dipeptide, a PAB motif, and an MMAE warhead. The DBCO group is a click chemistry handle which readily reacts with azide groups, while the Val-Cit is a protease-cleavable dipeptide which releases the MMAE warhead into cells via an elimination mechanism.
ODN 1982 sodium is a unmethylated oligodeoxyribonucleotide (ODN) with no CpG motif, and can be used to prepare DNA vaccines. ODN 1982 sodium inhibits R-848 signaling. ODN 1982 sequence: 5’-tccaggacttctctcaggtt-3’ .
Emapticap pegol sodium is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol sodium is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
244cis, a piperazine-containing ionizable cationic lipid, has been used to generate lipid nanoparticles (LNPs). LNPs containing 244cis and coated with mRNA reporter gene were specifically accumulated in mouse lungs compared with LNPs containing SM-102. Induces a decrease in serum chemokine (C-C motif) ligand 2 (CCL2) levels .
ODN 5328 (ODN 2395 Control) can be used as a sequence control for C-class ODN 2395. ODN 5328 shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
ODN 5328 (ODN 2395 Control) sodium can be used as a sequence control for C-class ODN 2395. ODN 5328 sodium shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
ODN 1982 is a unmethylated oligodeoxyribonucleotide (ODN) with no CpG motif, can be used to prepare DNA vaccines. ODN 1982 inhibits R-848 signaling. ODN 1982 sequence: 5’-tccaggacttctctcaggtt-3’ .
Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
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