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NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC)typeV isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for typeV, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
Satigrel (E5510) is a potent inhibitor of platelet aggregation. Satigrel inhibits collagen- and arachidonic acid-induced platelet aggregation through preventing thromboxane A2 synthesis by selective inhibition of the target enzyme, PGHS1, which exists in platelets. Satigrel inhibits PGHS1 (IC50: 0.081 μM) and PGHS2 (IC50: 5.9 μM). Satigrel is against Type III PDE, TypeV and Type II (IC50: 15.7 μM, 39.8 μM and 62.4 μM, respectively) .
Highly purified TypeV collagen, from bovine amnion (Bovine Amnion TypeV collagen, immunization grade) is an immune grade collagen derived from bovine amnion, which can stimulate the animal's immune system to produce specific antibodies against this collagen. Collagen is also a substrate for hydrolysis by MMPs .
Highly purified TypeV collagen, from mouse intestine (Mouse Type II collagen, immunization grade) is an immune grade collagen derived from mouse intestine, which can stimulate the animal's immune system to produce specific antibodies against this collagen. Collagen is also a substrate for hydrolysis by MMPs .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D/V654A is a mutant of KIT. KIT V559D/V654A Recombinant Human Active Protein Kinase is a recombinant KIT V559D/V654A protein that can be used to study KIT V559D/V654A-related functions .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V654A is a mutant of KIT. KIT V654A Recombinant Human Active Protein Kinase is a recombinant KIT V654A protein that can be used to study KIT V654A-related functions .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D/T670I is a mutant of KIT. KIT V559D/T670I Recombinant Human Active Protein Kinase is a recombinant KIT V559D/T670I protein that can be used to study KIT V559D/T670I-related functions .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D is a mutant of KIT. KIT V559D Recombinant Human Active Protein Kinase is a recombinant KIT V559D protein that can be used to study KIT V559D-related functions .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V560G is a mutant of KIT. KIT V560G Recombinant Human Active Protein Kinase is a recombinant KIT V560G protein that can be used to study KIT V560G-related functions .
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT D816V is a mutant of KIT. KIT D816V Recombinant Human Active Protein Kinase is a recombinant KIT D816V protein that can be used to study KIT D816V-related functions .
Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis .
Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
Tafamidis (Standard) is the analytical standard of Tafamidis. This product is intended for research and analytical applications. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
V-ATPase-IN-1 (Compound 3b-03) is a Vacuolar-type H +-ATPases (V-ATPase) inhibitor (IC50 = 194.80 μM) that can effectively target the V-ATPase subunit A (Kd = 0.803 μM). V-ATPase-IN-1 exhibits insecticidal activity against M. separata (LC50 = 2.64 mM) and contributes to research in the development of chemical insecticides .
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
Bafilomycin D is a specific inhibitor of vacuolar-type ATPase (V-ATPase). Bafilomycin D has antimicrobial, insecticidal, herbicidal and cytotoxic activity .
Tafamidis meglumine (Standard) is the analytical standard of Tafamidis meglumine. This product is intended for research and analytical applications. Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis .
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52 .
SMU-V18 is a vesicular stomatitis virus (VSV) inhibitor, with an EC50 of 6.2 μM. SMU-V18 inhibits VSV-GFP fluorescence intensity, viral mRNA/protein expression, and progeny virus replication. SMU-V18 interferes with early viral infection stages, also effective against wild-typeVSV (VSV-WT). SMU-V18 inhibits VSV-GFP in mouse tissues and prolongs survival. SMU-V18 can be used for the study of vesicular stomatitis virus (VSV) infection .
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range .
Anti-Rat TCR gamma/delta Antibody (V65) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to rat TCR gamma/delta. Anti-Rat TCR gamma/delta Antibody (V65) can deplete γδ T cells. Anti-Rat TCR gamma/delta Antibody (V65) can be used for the research of immunology .
Mogroside V is a the major active constituent of a traditional Chinese medicine Siraitiae Fructus. Mogroside V reduces the intracellular reactive oxygen species (ROS) levels and enhances mitochondrial function. Mogroside V has anti-oxidative, anti-diabetic and anti-carcinogenic effects. Mogroside V can be used for diabetic diseases research .
Mogroside V (Standard) is the analytical standard of Mogroside V. This product is intended for research and analytical applications. Mogroside V is a the major active constituent of a traditional Chinese medicine Siraitiae Fructus. Mogroside V reduces the intracellular reactive oxygen species (ROS) levels and enhances mitochondrial function. Mogroside V has anti-oxidative, anti-diabetic and anti-carcinogenic effects. Mogroside V can be used for diabetic diseases research .
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-typecalcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-typecalcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions .
sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively .
Concanamycin G has antifungal, antiviral, immunosuppressive, cytotoxic and other activities, and is a specific inhibitor of V-type ATPase (Ki=0.02 nM), which is an important tool for biochemical research .
Concanamycin F has antifungal, antiviral, immunosuppressive, cytotoxic and other activities, and is a specific inhibitor of V-type ATPase (Ki=0.02 nM), which is an important tool for biochemical research .
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
Mesenchymal-to-epithelial transition (MET) is a receptor tyrosine kinase for hepatocyte growth factor (HGF). MET overactivation is strongly associated with angiogenesis, cellular motility, growth, and invasion. Aberrant MET signaling can drive tumorigenesis in several cancer types through various molecular mechanisms, including MET amplification, MET exon 14 skipping mutation, MET overexpression, and MET fusions. MET L1195V is a mutant of MET. MET L1195V Recombinant Human Active Protein Kinase is a recombinant MET L1195V protein that can be used to study MET L1195V-related functions .
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H +-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research - .
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Gcase activator 2 (compound 14), a pyrrolo[2,3-b]pyrazine, is alos a β-Glucocerebrosidase (GCase) activator (EC50=3.8 μM). Gcase activator 2 induces GCase dimerizatio (both K-type and V-type). And Gcase activator 2 has low metabolic clearance in human and mouse .
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in
FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations .
AMG0347 is a transient receptor potential typeV1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm) .
Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155) .
Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer .
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild typeRET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
RET-IN-21 (compound 5) is a selective RET V804M inhibitor with the IC50 of 0.02 μM. RET-IN-21 does not inhibit the wild type isoforms of RET or KDR. RET-IN-21 has antitumor activity .
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild typeRET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia .
Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) .
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
Pacritinib (SB1518) is a potent inhibitor of both wild-typeJAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi . Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC) .
Neutral protease I (Dispase I) is a rapid, effective, gentle and neutral protease that can separate intact epidermis from the dermis. Neutral protease I can also separate intact epithelial sheets in culture from the substratum. Neutral protease I preserves the viability of the epithelial cells while cleaving the basement membrane zone region. Neutral protease I can also be used to prevent clumping in suspension cultures. Neutral protease I cleaves fibronectin and type IV collagen, but not laminin, typeV collagen, serum albumin, or transferrin .
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
Peptide P2.2, a non-ribosomal peptide, is an antimicrobial peptide. Peptide P2.2 has potent antibacterial activity with MIC50s of 4 and 32 μM for V. parahaemolyticus and V. alginolyticus, respectively. Peptide P2.2 increases synergistic antibacterial effects with antibiotics (such as Ofloxacin (HY-B0125) and Linezolid (HY-10394)) with negligible hemolytic activity. Peptide P2.2 disrupts bacterial membranes and increases permeability by modulating proteins involved in the type VI and III secretion systems. Peptide P2.2 can be used for bacterial infections research .
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
pan-KRAS-IN-18 (Compound 14-1) is a pan-KRAS inhibitor. pan-KRAS-IN-18 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS G12D, KRAS G12V and KRAS G12C) cancer cells. pan-KRAS-IN-18 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .
Pacritinib hydrochloride is a potent inhibitor of both wild-typeJAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
KRAS-IN-43 (Compound 9) is a pan-KRAS inhibitor with IC50 values of 0.15 μM, 0.14 μM, and 0.47 μM against KRAS G12V, KRAS G12C and wild-type KRAS, respectively. KRAS-IN-43 disrupts the interaction between KRAS and cRAF, and inhibits ERK phosphorylation. KRAS-IN-43 is promising for research of KRAS mutation-related cancers (such as pancreatic cancer, colorectal cancer, and lung cancer) .
HPMC (Hypromellose) (Type I, Viscosity: 400mPa.s) is a first-grade sodium alginate with an average viscosity of 400 mPa.s. Typically, a 1% w/v HPMC aqueous solution has a viscosity of 20-400mPa.s (20-400cp) at 20°C. The viscosity of HPMC may vary depending on concentration, pH, temperature, or the presence of metal ions. Viscosity decreases at pH values above 10 .
Pacritinib (SB1518) citrate is a potent inhibitor of both wild-typeJAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib citrate also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-typeJAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
A-425619 is an orally active and selective transient receptor potential typeV1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca 2+ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury .
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines .
FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC50: 4.7 μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
HIV-1-IN-85 is an orally active HIV-1 inhibitor (IC50 = 72 nM). HIV-1-IN-85 exhibits strong inhibitory activity against wild-type (WT) HIV-1 and NNRTI-resistant single mutant strains (L100I, K103N, Y181C, Y188L, E138K) and moderate efficacy against double mutant strains (F227L+V106A, RES056). HIV-1-IN-85 shows good in vivo safety in ICR mice. HIV-1-IN-85 can be used for the study of HIV-1 infection .
PROTAC pan-KRAS degrader-1 is a pan-KRASPROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
Poly[bis(4-phenyl)(2,4,6-trimethylphenyl)amine] is a poly(triarylamine) that is an organic p-type semiconductor with hole mobilities ranging from 10 3 to 10 2 cm 2/V/s, which significantly improves carrier mobility. This stable, glassy polymer has an ionization potential suitable for thick film diodes. Committed to providing green alternatives that meet one or more of the 12 principles of green chemistry, this material falls into the enabling category of green alternatives, in line with the principle of "energy efficient design". In addition, while hole transport organic materials like these ensure optimal energy level alignment with the absorber layer for efficient charge collection, they can be susceptible to degradation under ambient conditions.
XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria .
HPMC (Hypromellose) (Type I, Viscosity: 400mPa.s) is a first-grade sodium alginate with an average viscosity of 400 mPa.s. Typically, a 1% w/v HPMC aqueous solution has a viscosity of 20-400mPa.s (20-400cp) at 20°C. The viscosity of HPMC may vary depending on concentration, pH, temperature, or the presence of metal ions. Viscosity decreases at pH values above 10 .
Highly purified TypeV collagen, from bovine amnion (Bovine Amnion TypeV collagen, immunization grade) is an immune grade collagen derived from bovine amnion, which can stimulate the animal's immune system to produce specific antibodies against this collagen. Collagen is also a substrate for hydrolysis by MMPs .
Highly purified TypeV collagen, from mouse intestine (Mouse Type II collagen, immunization grade) is an immune grade collagen derived from mouse intestine, which can stimulate the animal's immune system to produce specific antibodies against this collagen. Collagen is also a substrate for hydrolysis by MMPs .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-typecalcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-typecalcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
Peptide P2.2, a non-ribosomal peptide, is an antimicrobial peptide. Peptide P2.2 has potent antibacterial activity with MIC50s of 4 and 32 μM for V. parahaemolyticus and V. alginolyticus, respectively. Peptide P2.2 increases synergistic antibacterial effects with antibiotics (such as Ofloxacin (HY-B0125) and Linezolid (HY-10394)) with negligible hemolytic activity. Peptide P2.2 disrupts bacterial membranes and increases permeability by modulating proteins involved in the type VI and III secretion systems. Peptide P2.2 can be used for bacterial infections research .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
Anti-Rat TCR gamma/delta Antibody (V65) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to rat TCR gamma/delta. Anti-Rat TCR gamma/delta Antibody (V65) can deplete γδ T cells. Anti-Rat TCR gamma/delta Antibody (V65) can be used for the research of immunology .
HY-P990958 is an T cell receptor germline-encoded variable chain Vβ6/β10-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001) .
Bafilomycin D is a specific inhibitor of vacuolar-type ATPase (V-ATPase). Bafilomycin D has antimicrobial, insecticidal, herbicidal and cytotoxic activity .
Mogroside V is a the major active constituent of a traditional Chinese medicine Siraitiae Fructus. Mogroside V reduces the intracellular reactive oxygen species (ROS) levels and enhances mitochondrial function. Mogroside V has anti-oxidative, anti-diabetic and anti-carcinogenic effects. Mogroside V can be used for diabetic diseases research .
Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H +-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research - .
Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi . Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC) .
Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria .
Mogroside V (Standard) is the analytical standard of Mogroside V. This product is intended for research and analytical applications. Mogroside V is a the major active constituent of a traditional Chinese medicine Siraitiae Fructus. Mogroside V reduces the intracellular reactive oxygen species (ROS) levels and enhances mitochondrial function. Mogroside V has anti-oxidative, anti-diabetic and anti-carcinogenic effects. Mogroside V can be used for diabetic diseases research .
Concanamycin G has antifungal, antiviral, immunosuppressive, cytotoxic and other activities, and is a specific inhibitor of V-type ATPase (Ki=0.02 nM), which is an important tool for biochemical research .
Concanamycin F has antifungal, antiviral, immunosuppressive, cytotoxic and other activities, and is a specific inhibitor of V-type ATPase (Ki=0.02 nM), which is an important tool for biochemical research .
Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
ATP6V1F is an important subunit of the vacuolar (H+)-ATPase (V-ATPase) V1 complex and is an important component of this enzyme's role in cellular pH regulation. It forms a catalytic AB heterodimer and peripheral stem that plays a role in ATP hydrolysis. ATP6V1F Protein, Human is the recombinant human-derived ATP6V1F protein, expressed by E. coli , with tag free.
VISTA/B7-H5 Protein is a type I transmembrane protein expressed primarily in white blood cells that inhibits T cell function. VISTA/B7-H5 Protein promotes embryonic stem cell differentiation by inhibiting BMP4 signaling and stimulates MMP14 mediated MMP2 activation. VISTA/B7-H5 Protein is highly expressed in tumors. VISTA/B7-H5 Protein, Mouse (159a.a, HEK293, His) is the recombinant mouse-derived VISTA/B7-H5 protein, expressed by HEK293 , with C-6*His labeled tag.
The PRDX5 protein (or Peroxiredoxin-5) plays a critical role as a thiol-specific peroxidase that reduces hydrogen peroxide and organic hydroperoxides. This enzyme activity is essential for cells to defend against oxidative stress and detoxify peroxides. PRDX5/Peroxiredoxin-5 Protein, Human (HEK293, His) is the recombinant human-derived PRDX5/Peroxiredoxin-5 protein, expressed by HEK293 , with N-6*His labeled tag.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (HEK293, V474I, G670E, His) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-6*His labeled tag and V474I, G670E mutation.
ATP6V1F is an important subunit of the vacuolar (H+)-ATPase (V-ATPase) V1 complex and is an important component of this enzyme's role in cellular pH regulation. It forms a catalytic AB heterodimer and peripheral stem that plays a role in ATP hydrolysis. ATP6V1F Protein, Human (GST) is the recombinant human-derived ATP6V1F protein, expressed by E. coli , with N-GST labeled tag.
The PCSK9 protein is an important regulator of plasma cholesterol homeostasis, affecting LDL receptor family members such as LDLR and VLDLR. It promotes their intracellular degradation and enhances hepatic LDLR degradation through non-proteolytic mechanisms. PCSK9 Protein, Human (Biotinylated, V474I, G670E, HEK293, His-HA-Avi) is the recombinant human-derived PCSK9 protein, expressed by HEK293 , with C-Avi, C-HA, C-8*His labeled tag and V474I, G670E mutation.
The SIRP α V4/CD172a protein is an immunoglobulin-like cell surface receptor for CD47 that acts as a docking protein to facilitate the translocation of PTPN6, PTPN11, and other partners to the plasma membrane. It supports the adhesion of cerebellar neurons, promotes neurite growth, and promotes glial cell attachment. SIRP alpha V5/CD172a Protein, Human (HEK293, His, Avi) is the recombinant human-derived SIRP alpha V5/CD172a protein, expressed by HEK293, with C-His and C-Avi labeled tag.
Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-typeJAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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