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Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs .
BC-1258, an F-box/LRR-repeat protein 2 (FBXL2) activator, can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells, and profoundly inhibits tumor formation in mice .
WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazepinone-based WD repeat domain 5 (WDR5) inhibitor. WDR5-IN-7 can be used for the research of anti-cancer .
OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs .
NSC45586 sodium is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 sodium targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 sodium can activate AKT in neurons .
NSC45586 is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 can activate AKT in neurons .
PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD) .
OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tau protein .
Toringin, a bioflavonoid, is isolated from the bark of Docyniopsis tschonoski. Toringin progressively decreases not only the cis-effect of the expanded CTG repeats but cytotoxicity as well. Exposure to isosakuranetin, Toringin rescues PC12 neuronal cells. Flavonoids are efficacious for ameliorating the RNA gain of function caused by expanded CTG repeats, and have various biological activities and beneficial actions against cancers, coronary heart disease, among other pathologies .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tau protein aggregation and is mapped to the third microtubule-binding repeat region of the tau protein .
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 .
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 .
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo .
di-Ellipticine-RIBOTAC is a dual-function small molecule that reduces c9ALS/FTD r(G4C2) repeat expansion in vitro and in vivo amyotrophic lateral sclerosis (ALS ) models.
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
ssRNA40 (sodium) is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. ssRNA40 is a uridine-rich ssRNA derived from the HIV-1 long terminal repeat on activation of NK cells via TLR7/8[1][2].
IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively . IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM .
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
Tau Peptide (255-314) (Repeat 2 Domain) (human) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
Methyl gerfelin inhibits osteoclast differentiation by binding 3 major cellular proteins: glyoxalase 1 (GLO1), sterol binding protein 2 (SCP2), and small glutamine-rich tetratricopeptide repeat containing protein A (SGTA). Methyl gerfelin is a potent GLO1 inhibitor related to the flavonoid class .
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
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 .
WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity .
Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types .
WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity .
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area .
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
rTRD01 is a TDP-43 ligand that binds to TDP-43’s RRM1 and RRM2 domains (Kd=89 uM for TDP-43102–269). rTRD01 partially disrupts TDP-43’s interaction with the hexanucleotide RNA repeat of the disease-linked c9orf72 gene. rTRD01 can be used for the research of neurodegenerative diseases .
MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier .
LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier .
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
Chrexanthomycin C is an orally active marine natural product with remarkable bioactivities. Chrexanthomycin C has binding affinity for DNA (G4C2) 4 G4 with a Kd value of 2.8 mM. Chrexanthomycin C can be used for the research of neurodegenerative disease such as amyotrophic lateral sclerosis (ALS) .
Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tau protein .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tau protein aggregation and is mapped to the third microtubule-binding repeat region of the tau protein .
Uty HY Peptide (246-254), derived from the ubiquitously transcribed tetratricopeptide repeat gene on the Y chromosome (UTY) protein as an H-Y epitope, H-YD b, is a male-specific transplantation antigen H-Y .
Uty HY Peptide (246-254) TFA, derived from the ubiquitously transcribed tetratricopeptide repeat gene on the Y chromosome (UTY) protein as an H-Y epitope, H-YD b, is a male-specific transplantation antigen H-Y .
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.
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.
Interphotoreceptor Retinoid Binding Protein Fragment (IRBP), a 20-residue peptide and a major pathogenic epitope, is present in the first homologous repeat of the interphotoreceptor retinoid binding protein peptide (IRBP 161–180), which can induce posterior uveitis (EAU) .
Interphotoreceptor Retinoid Binding Protein Fragment (IRBP) TFA, a 20-residue peptide and a major pathogenic epitope, is present in the first homologous repeat of the interphotoreceptor retinoid binding protein peptide (IRBP 161–180), which can induce posterior uveitis (EAU) .
Tau Peptide (337-368) (Repeat 4 Domain) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Acetyl-Tau Peptide (244-274) (Repeat 1 Domain) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (255-314) (Repeat 2 Domain) (human) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
C34 peptide is a biological active peptide. (This C34 peptide, also known as HR2, belongs to the helical region of gp41 of HIV, C-terminal heptad repeat 2 (HR2) defined as C helix or C peptide. It is known that HIV-1 enters cells by membrane fusion, C34 gp41 peptide is a potent inhibitors of HIV-1 fusion.)
Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area .
Toringin, a bioflavonoid, is isolated from the bark of Docyniopsis tschonoski. Toringin progressively decreases not only the cis-effect of the expanded CTG repeats but cytotoxicity as well. Exposure to isosakuranetin, Toringin rescues PC12 neuronal cells. Flavonoids are efficacious for ameliorating the RNA gain of function caused by expanded CTG repeats, and have various biological activities and beneficial actions against cancers, coronary heart disease, among other pathologies .
Chrexanthomycin C is an orally active marine natural product with remarkable bioactivities. Chrexanthomycin C has binding affinity for DNA (G4C2) 4 G4 with a Kd value of 2.8 mM. Chrexanthomycin C can be used for the research of neurodegenerative disease such as amyotrophic lateral sclerosis (ALS) .
EDIL3 Protein enhances endothelial cell adhesion by interacting with the alpha-v/beta-3 integrin receptor, while also inhibiting the formation of vascular-like structures. Its role suggests involvement in the regulation of vascular morphogenesis during embryonic development. EDIL3 Protein, Human (HEK293, His) is the recombinant human-derived EDIL3 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of EDIL3 Protein, Human (HEK293, His) is 457 a.a., with molecular weight of ~56 kDa.
EDIL3 Protein enhances endothelial cell adhesion by interacting with the alpha-v/beta-3 integrin receptor, while also inhibiting the formation of vascular-like structures. Its role suggests involvement in the regulation of vascular morphogenesis during embryonic development. EDIL3 Protein, Human (HEK293, His, solution) is the recombinant human-derived EDIL3 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of EDIL3 Protein, Human (HEK293, His, solution) is 457 a.a., with molecular weight of ~56 kDa.
rMuLeucine-rich repeats and immunoglobulin-like domains protein 1/LRIG1, His; Leucine-rich repeats and immunoglobulin-like domains protein 1; LIG-1; Lrig1
The LRIG1 protein acts as a negative feedback regulator of receptor tyrosine kinase signaling by promoting receptor ubiquitination and accelerating intracellular degradation. Its extracellular LRR and Ig-like domains can interact with EGFR/ERBB1, ERBB2, ERBB3 and ERBB4. LRIG1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived LRIG1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of LRIG1 Protein, Mouse (HEK293, His) is 760 a.a., with molecular weight of ~94.0 kDa.
ANKFY1 is a proposed Rab5 effector that critically participates in endosomal dynamics by binding to PI(3)P, promoting homotypic early endosomal fusion and participating in heterotypic fusion. It plays a crucial role in macropinocytosis, is dependent on Rab5-GTP, and is essential for the correct localization of activated tyrosine kinase receptors such as PDGFRB. ANKFY1 Protein, Human (Sf9, His, Strep) is the recombinant human-derived ANKFY1 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of ANKFY1 Protein, Human (Sf9, His, Strep) is 1168 a.a., .