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Efalizumab is a targeted Tcell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits Tcellactivation, cutaneous Tcell trafficking, and Tcell adhesion to keratinocytes, can be used for plaque psoriasis research .
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress Tcellactivation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activatedTcells (NFAc) .
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on Tcellactivation .
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 +Tcellactivation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
PVD-06 is a selective PTPN2 degrader (PTPN2/PTP1B selectivity index >60-fold) and induces PTPN2 degradation in a ubiquitination- and proteasome-dependent manner. PVD-06 promotes Tcellactivation and amplifies IFN-γ-mediated cytotoxicity. PVD-06 has anticancer activity .
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activatedTcells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity .
Heraclenin, a natural furanocoumarin, significantly inhibits Tcell receptor-mediated proliferation in human primary Tcells in a concentration-dependent manner by targeting nuclear factor of activatedT-cells (NFAT) .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes Tcells, decreases Tcellactivation, inhibites Tcell proliferation and enriches naïve and bona fide regulatory Tcells .
AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity .
PD-L1/PD-1-IN-1 (compound 8j) is a potent inhibitor of PD-L1/PD interaction, with IC50 < 1 nM. PD-L1/PD-1-IN-1 plays an important role in anti-tumor research .
Teclistamab is a human bispecific antibody to BCMA and CD3 that recognizes BCMA on target cells and CD3 on Tcells and induces Tcell-mediated cytotoxicity leading to Tcellactivation and subsequent target cell lysis. Teclistamab can be used in studies of diseases related to multiple myeloma (MM) .
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293Tcells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells .
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activatedT lymphocyte–mediated immune responses in Con A-activatedTcells. Trichomide A have the potential for the research of immune-related skin diseases .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on Tcells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces Tcellactivation and proliferation .
Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on Tcells. Glofitamab leads to T-cellactivation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell lymphoma .
Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cellactivation. Cbl-b-IN-15 activatesTcell function with EC50=0.41 μM .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to Tcells. Phospholipid PL1 could induce the activation of various immune cells, including Tcells and dendritic cells (DCs) in order to boost antitumor immunity .
Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody against OX40. Among them, OX40 is a member of the TNF receptor superfamily expressed on activated and memory Tcell subsets and T regulatory cells .
HDMAPP triammonium is a potent phosphoantigen in the ammonium form and the pyrophosphate form of (E)-HDMAPP. HDMAPP is also a potent activator of γδ Tcells and can induce Tcell stimulation in vitro (EC50=0.39 nM, TNF-α) .
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/Tcell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells . DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance .
11R-VIVIT is a cell-permeable nuclear factor of activatedTcells (NFAT) inhibitor. 11R-VIVIT can be used for the research of podocyte and diabetic nephropathy .
DFHBI-1T is a membrane-permeable RNA aptamers-activated fluorescence probe (ex/em=472 nm/507 nm). DFHBI-1T binds to RNA aptamers (Spinach, Spinach2, iSpinach, and Broccoli) and causes specific fluorescence and lower background fluorescence. DFHBI-1T is used to image RNA in live cells .
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activatedT-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
KV1.3-IN-1 (Compound trans-18) is a KV1.3 channel inhibitor (IC50: 230 nM and 26.12 nM in Ltk?cells and PHA-activatedT-lymphocytes respectively). KV1.3-IN-1 impairs intracellular Ca 2+ signaling. KV1.3-IN-1 inhibits T-cellactivation, proliferation, and colony formation .
AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome .
(E)-C-HDMAPP ammonium, is a potent phosphoantigen in ammonium form as well as a pyrophosphonate form of (E)-HDMAPP. (E)-C-HDMAPP is also an effective activator of γδ-Tcells, induces T-cell stimulatory responses in vitro (EC50=0.91 nM for TNF-α release) .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive Tcell polarization to the anti-inflammatory Treg phenotype .
11R-VIVIT TFA is a cell-permeable nuclear factor of activatedTcells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy .
HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells .
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activatedTcells, NK cells, B cells and plasmacytoid dendritic cells .
CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of Tcells .
CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of Tcells .
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activatedTcells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
PKM2 activator 7 (Compd B4) is a PKM2activator with the AC50 of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting Tcell growth in mouse colitis model .
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cellactivation .
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce Tcell-mediated killing of GPRC5D-expressing MM cells through Tcell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
Eftilagimod alfa (IMP321) is a recombinant LAG-3Ig fusion protein that binds to MHC class II. Eftilagimod alfa mediates antigen-presenting cell (APC) activation followed by CD8 T-cellactivation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
PD-1/PD-L1-IN-27 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 134 nM. PD-1/PD-L1-IN-27 shows antitumor effects with low Tcell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8 +Tcells and reduces Tcell exhaustion .
INX-SM-56 is a cytotoxin that can be used for the synthesis of anti-VISTA antibody agent conjugate. VISTA: V-region Immunoglobulin-containing Suppressor of TcellActivation .
AS2863619 enables conversion of antigen-specific effector/memory Tcells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene .
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cellactivation and promotes the proliferation of CD4 +T and CD8 +Tcells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ Tcell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of Tcell subsets, which leads to NF-κBactivation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent .
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cellactivator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis .
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance Tcellactivation and antitumor immunity .
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cellActivation) monoclonal antibody. Onvatilimab has an anti-tumor activity .
AS2863619 free base enables conversion of antigen-specific effector/memory Tcells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene .
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cellactivation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model .
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances Tcell infiltration and antitumor Tcell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research .
KRN2 is a selective inhibitor of nuclear factor of activatedTcells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis .
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activateAMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human Tcells, can also be used in studies of cancer and T-cell apoptosis dysregulation .
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired Tcell function and often co-expressed with PD-1, that enhances Tcell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat Tcell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate Tcellactivation .
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activatesAMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
Evunzekibart (ATOR-1017) is an Fc-γ receptor conditional 4-1BB agonist and IgG4-type antibody. Evunzekibart can be used as monotherapy or in combination with anti-PD1 to exert anticancer activity.
NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTK C481S in cells. NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates Tcellactivation and increases IL-2 production in primary human TCells .
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cellactivation .
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activatedTcells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis .
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activatesTcells in NSG mice. Bavunalimab can be used for the research of cancer .
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activatedTcells toward CXCL11 .
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cellactivation .
KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca 2+ signaling in Jurkat Tcells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat Tcells .
4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce Tcell apoptosis independent of caspase receptor activation, and can activate the mitochondrial death pathway by producing reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide can be used in the study of rheumatoid arthritis and autoimmune diseases .
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively . Tamoxifen activatesautophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
Nemvaleukin alfa (ALKS 4230) is a IL-2 fusion protein that selectively binds to intermediate-affinity IL-2R. Nemvaleukin alfa is an activator of NK and effector Tcells. Nemvaleukin alfa can be used for research of cancer .
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
20(S)-Hydroxycholesterol (Standard) is the analytical standard of 20(S)-Hydroxycholesterol. This product is intended for research and analytical applications. 20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activatedTcell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research .
Sp-8-Br-cAMPS sodium is a cAMP analog, which performs a protein kinase A (PKA) activating activity with EC50 of 360 nM. Sp-8-Br-cAMPS sodium inhibits proliferation of Tcells and the haemocyte non-self response in Lepidoptera larve .
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific Tcells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activatingcaspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress. LYP-IN-3 activatesT-cell and inhibits M2 macrophage polarization, but upregulates PD-1/PD-L1 expression. LYP-IN-3 can be leveraged with PD-1/PD-L1 inhibitor, for futher cancer immunotherapy .
L-Kynurenine-13C10 (sulfate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive Tcell polarization to the anti-inflammatory Treg phenotype .
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
5-A-RU-PABC-Val-Cit-Fmoc is the proagent of 5-A-RU . 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cellsactivator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways .
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM . OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis .
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively . Tamoxifen Citrate activatesautophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κBactivation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1)activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia .
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activatedT-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat[1]. Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses Tcell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2[2][3][4][5].
Tamoxifen (Standard) is the analytical standard of Tamoxifen. This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activatesautophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain) . OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner . OSU-T315 causes cell death through apoptosis and autophagy .
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating Tcellsactivation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer .
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting Tcell infiltration and activation .
QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1cell-mediated immune responses through action on antigen presenting cells (APCs) and Tcells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18 .
HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), Tcells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1) .
HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), Tcells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38) .
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cellactivation- .
CD19 CAR mRNA will express CD19 car protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
CD19 CAR circRNA will express CD19 car protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
4-Hydroperoxy Cyclophosphamide-d4 is the deuterium labeled 4-Hydroperoxy cyclophosphamide. 4-Hydroperoxy cyclophosphamide is the active metabolite form of the proagent Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces Tcell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders[1][2].
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activatesAMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without Tcellactivation or toxicity .
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4 +Tcellactivation. RDN2150 can be used for research of psoriasis .
ω-Conotoxin Bu8 is a ω-conotoxin, which consists of 25 amino acid residues and three disulfide bridges. ω-Conotoxin Bu8 selectively and potently inhibits depolarization-activated Ba2+ currents mediated by rat CaV2.2 expressed in HEK293Tcells (IC50= 89 nM) .
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a Tcellsactivator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, Tcells and dendritic cells .
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote Tcell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cellactivation- .
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activatesautophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis .
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit Tcellactivation by inhibiting IL-2 expression .
PRO-F is a photoactivable H2S donor with ROS scavenging ability. PRO-F can be activated by light to produce fluorescent signal, for real-time tracking of released H2S. PRO-F activation doesn’t consume endogenous substances. deliver H2S in an intracellular environment to protect cells from excessive reactive oxygen species (ROS) induced damage. PRO-F shows enhancement on chronic wound healing, researched in diabetic models as well .
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered Tcellactivation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered Tcellactivation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a Tcell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances Tcell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a “super-cooling agent” . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response .
RDN2150 (Compound 25) TFA is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 TFA covalently binds to the C346 residue of ZAP-70. RDN2150 TFA inhibits the expression of CD25 and CD69, and inhibits CD4 +Tcellactivation. RDN2150 TFA can be used for research of psoriasis .
Plecanatide (Standard) is the analytical standard of Plecanatide. This product is intended for research and analytical applications. Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis .
Agrimol B, a polyphenol, is an orally active and potent SIRT1activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27 .
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cellactivation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al .
C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote Tcell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ Tcells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and Tcellactivation .
ODN 2216 is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4 +Tcells .
CD19 car circRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car circRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car circRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
CD19 car mRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car mRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car mRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
ODN?2216 sodium is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN?2216 sodium induces high amounts of IFN-α and IFN-β. ODN 2216 sodium induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 sodium stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 sodium can activate NK cells and promote IFN-γ production of TCR-triggered CD4 +Tcells .
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other Tcell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
AL-8810 is a potent and selective antagonist of the PGF 2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The Ki of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG) .
(R)-Phe-A110/B319, a hapten, is a selective binder to tumor-associated antigens. (R)-Phe-A110/B319 has a 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α PI3K complex. (R)-Phe-A110/B319 can be used for the research of conditional chimeric antigen receptor T (CAR-T) cellactivation and tumor targeting .
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ Tcells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on Tcellactivation .
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPKactivation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity .
PD-1/PD-L1-IN-25 (compound D2) is an inhibitor of PD-1/PD-L1 interaction with an IC50 value of 16.17 nM. PD-1/PD-L1-IN-25 activates the antitumor immunity of Tcells efficiently in PBMCs. PD-1/PD-L1-IN-25 can be used for the research of cancer .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study Tcell-mediated autoimmune diseases .
PD-1-IN-25 (compound 43) is a potent PD-1/PD-L1 interaction inhibitor with an IC50 value of 10.2 nM in the HTRF assay. PD-1-IN-25 can promote CD8+ Tcellactivation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth .
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of Tcells .
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activatingTcells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote Tcellactivation and can be used in cancer immunity research .
PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ Tcells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases .
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cellactivation and has the potential for chronic inflammatory and autoimmune diseases research .
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of Tcells .
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 .
PD-1/PD-L1-IN-33 (Compound N11) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-33 inhibits PD-1 and PD-L1 interaction with an IC50: 6.3 nM. PD-1/PD-L1-IN-33 promotes T-cell proliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity .
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cellactivation and has the potential for chronic inflammatory and autoimmune diseases research .
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1 . BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on Tcellactivation .
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits Tcellactivation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing Tcells.IHMT-PI3K-455 is used in cancer research .
DFHBI-1T is a membrane-permeable RNA aptamers-activated fluorescence probe (ex/em=472 nm/507 nm). DFHBI-1T binds to RNA aptamers (Spinach, Spinach2, iSpinach, and Broccoli) and causes specific fluorescence and lower background fluorescence. DFHBI-1T is used to image RNA in live cells .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to Tcells. Phospholipid PL1 could induce the activation of various immune cells, including Tcells and dendritic cells (DCs) in order to boost antitumor immunity .
CD19 car circRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car circRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car circRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
CD19 car mRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car mRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car mRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cell proliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress Tcellactivation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activatedTcells (NFAc) .
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activatedT lymphocyte–mediated immune responses in Con A-activatedTcells. Trichomide A have the potential for the research of immune-related skin diseases .
Tetanus Toxin (830–844) is a biological active peptide. (tetanus toxin-derived peptide TT830–844 CD4+ T-cell epitope. This promiscuous CD4+ T-cell epitope can bind to a wide range of HLA–DRB molecules and is thus expected to activate CD4+ T-cell responses in a large part of the human population)
11R-VIVIT is a cell-permeable nuclear factor of activatedTcells (NFAT) inhibitor. 11R-VIVIT can be used for the research of podocyte and diabetic nephropathy .
[Gln144]-PLP (139-151) is an experimental antigen used to study Tcells respond to both autoantigens and cross-reactive non-autoantigens. [Gln144]-PLP (139-151) activatesTcells by binding to T-cell Receptor (TCR), which triggers an immune response. [Gln144]-PLP (139-151) can be used to study the regulation of autoimmune diseases .
11R-VIVIT TFA is a cell-permeable nuclear factor of activatedTcells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy .
M133 peptide is a coronavirus-specific CD4 Tcell epitope. M133 peptide is immunodominant in mice infected with the neurotropic coronavirus (the JHM strain of mouse hepatitis virus). M133 peptide forms a complex with MHC II molecules, which is recognized by specific TCRs, thereby activating CD4 Tcells .
KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca 2+ signaling in Jurkat Tcells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat Tcells .
[Leu144]-PLP (139-151) (L144-PLP(139-151)) is a peptide ligand of Tcell receptor. [Leu144]-PLP (139-151) is a TCR antagonist for encephalitogenic Th1 clones, blocking their activation .
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis .
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cellactivation- .
ω-Conotoxin Bu8 is a ω-conotoxin, which consists of 25 amino acid residues and three disulfide bridges. ω-Conotoxin Bu8 selectively and potently inhibits depolarization-activated Ba2+ currents mediated by rat CaV2.2 expressed in HEK293Tcells (IC50= 89 nM) .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cellactivation- .
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis .
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a Tcell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
Plecanatide (Standard) is the analytical standard of Plecanatide. This product is intended for research and analytical applications. Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis .
Cy3-Ova (323-339) is an Cy3 labled OVA Peptide (323-339) (HY-P0286). Cy3 is a fluorescent dye belonging to the Cyanine family and is a fluorescent light product of Cy5. Cyanine is commonly used in fluorescence microscopy, cell imaging, and molecular biology experiments. OVA Peptide (323-339) represents the T and B cell epitopes of ovalbumin (OVA). OVA Peptide (323-339) has limited immunogenic efficacy in activating OVA-sensitized and attacked mouse spleen cells .
β-Interleukin I (163-171), human, an immunostimulatory fragment of human IL-1β peptide, is a Tcellactivator. β-Interleukin I (163-171), human is not an IL-1R-binding domain of IL-1β. β-Interleukin I (163-171), human is a potent adjuvant that enhances the immune response in a variety of exptl. situations .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study Tcell-mediated autoimmune diseases .
Efalizumab is a targeted Tcell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits Tcellactivation, cutaneous Tcell trafficking, and Tcell adhesion to keratinocytes, can be used for plaque psoriasis research .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes Tcells, decreases Tcellactivation, inhibites Tcell proliferation and enriches naïve and bona fide regulatory Tcells .
Teclistamab is a human bispecific antibody to BCMA and CD3 that recognizes BCMA on target cells and CD3 on Tcells and induces Tcell-mediated cytotoxicity leading to Tcellactivation and subsequent target cell lysis. Teclistamab can be used in studies of diseases related to multiple myeloma (MM) .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on Tcells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces Tcellactivation and proliferation .
Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on Tcells. Glofitamab leads to T-cellactivation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell lymphoma .
Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody against OX40. Among them, OX40 is a member of the TNF receptor superfamily expressed on activated and memory Tcell subsets and T regulatory cells .
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/Tcell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activatedTcells, NK cells, B cells and plasmacytoid dendritic cells .
Telazorlimab (GBR-830) is a humanized monoclonal antibody against OX40 costimulatory receptor on activatedTcells. Telazorlimab can be used for the research of autoimmune diseases .
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce Tcell-mediated killing of GPRC5D-expressing MM cells through Tcell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
Eftilagimod alfa (IMP321) is a recombinant LAG-3Ig fusion protein that binds to MHC class II. Eftilagimod alfa mediates antigen-presenting cell (APC) activation followed by CD8 T-cellactivation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cellActivation) monoclonal antibody. Onvatilimab has an anti-tumor activity .
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances Tcell infiltration and antitumor Tcell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research .
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired Tcell function and often co-expressed with PD-1, that enhances Tcell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
Pateclizumab (MLTA3698A) is a humanized antibody against lymphotoxin α (LTα), a transiently expressed cytokine on activated B and Tcells (Th1, Th17), which are implicated in rheumatoid arthritis (RA) pathogenesis .
Evunzekibart (ATOR-1017) is an Fc-γ receptor conditional 4-1BB agonist and IgG4-type antibody. Evunzekibart can be used as monotherapy or in combination with anti-PD1 to exert anticancer activity.
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cellactivation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activatesTcells in NSG mice. Bavunalimab can be used for the research of cancer .
Ivuxolimab is an OX40 (also known as CD134; TNFRSF4) agonist monoclonal antibody. OX40 is a costimulatory receptor expressed on activated CD4 + and CD8 +Tcells. Ivuxolimab shows antitumor activity, with potential immunostimulatory activity .
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cellactivation .
Nemvaleukin alfa (ALKS 4230) is a IL-2 fusion protein that selectively binds to intermediate-affinity IL-2R. Nemvaleukin alfa is an activator of NK and effector Tcells. Nemvaleukin alfa can be used for research of cancer .
Tregalizumab is a humanized anti-human CD4 monoclonal antibody (IgG1 type) that selectively activates the suppressive properties of regulatory Tcells (Tregs) in vitro. Tregalizumab can be used in the research of autoimmune diseases (resulting from insufficient Treg activity) and allergies .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activatedT-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
Lorukafusp alfa (14.18 mAb; hu14.18-IL2) is an immunocytokine consisting of the humanized 14.18 anti-GD2 mAb linked to IL210. Lorukafusp alfa has activity mediated by activation of antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity via the binding of hu14.18-IL2 to GD2 on the tumor cell surface, followed by binding to Fc receptors on effector cells along with activation of NK and Tcells via IL2 receptor binding. Lorukafusp alfa has anti-tumor activity .
Puxitatug is an immunoglobulin G1-κ, anti-[Homo sapiens VTCN1 (Vset domain containing Tcellactivation inhibitor 1, B7 family member H4, B7H4, B7-H4)] Homo sapiens monoclonal antibody .
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress Tcellactivation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activatedTcells (NFAc) .
Heraclenin, a natural furanocoumarin, significantly inhibits Tcell receptor-mediated proliferation in human primary Tcells in a concentration-dependent manner by targeting nuclear factor of activatedT-cells (NFAT) .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive Tcell polarization to the anti-inflammatory Treg phenotype .
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activatedTcells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cellactivation .
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of Tcell subsets, which leads to NF-κBactivation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent .
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cellactivator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis .
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat Tcell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
20(S)-Hydroxycholesterol (Standard) is the analytical standard of 20(S)-Hydroxycholesterol. This product is intended for research and analytical applications. 20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κBactivation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1)activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia .
QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1cell-mediated immune responses through action on antigen presenting cells (APCs) and Tcells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18 .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activatesAMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, Tcells and dendritic cells .
Agrimol B, a polyphenol, is an orally active and potent SIRT1activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27 .
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ Tcells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ Tcells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote Tcellactivation and can be used in cancer immunity research .
The CD27/TNFRSF7 protein is predicted to have endopeptidase inhibitor activity, be ethanol responsive, and be membrane localized. Its ortholog of human CD27 has been implicated in lymphoproliferative syndrome 2, emphasizing immune system regulation. CD27/TNFRSF7 Protein, Rat (HEK293, Fc) is the recombinant rat-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of CD27/TNFRSF7 Protein, Rat (HEK293, Fc) is 183 a.a., with molecular weight of 60-70 kDa.
The CD27/TNFRSF7 protein is a receptor for CD70/CD27L and may ensure the survival of activated T cells, suggesting that it plays a crucial role in immune responses. Its association with SIVA1 suggests a regulatory function in the apoptotic pathway. CD27/TNFRSF7 Protein, Human (sf9, His) is the recombinant human-derived CD27/TNFRSF7 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of CD27/TNFRSF7 Protein, Human (sf9, His) is 173 a.a., with molecular weight of ~27 kDa.
The CD27/TNFRSF7 protein is a receptor for CD70/CD27L and may ensure the survival of activated T cells, suggesting that it plays a crucial role in immune responses. Its association with SIVA1 suggests a regulatory function in the apoptotic pathway. CD27/TNFRSF7 Protein, Human (HEK293, Fc) is the recombinant human-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-rFc labeled tag. The total length of CD27/TNFRSF7 Protein, Human (HEK293, Fc) is 173 a.a., with molecular weight of ~63 kDa.
CD27/NFRSF7 Protein acts as a receptor for CD70/CD27L, supporting activated T-cell survival and potentially influencing apoptosis through interactions with SIVA1. It forms homodimers and engages with SIVA1 and TRAF2, indicating diverse roles in cellular processes. CD27/TNFRSF7 Protein, Mouse (HEK293, His) is the recombinant mouse-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-His labeled tag. The total length of CD27/TNFRSF7 Protein, Mouse (HEK293, His) is 159 a.a., with molecular weight of ~35 KDa.
The CD27/TNFRSF7 protein is a receptor for CD70/CD27L and may ensure the survival of activated T cells, suggesting that it plays a crucial role in immune responses. Its association with SIVA1 suggests a regulatory function in the apoptotic pathway. CD27/TNFRSF7 Protein, Human (Biotinylated, sf9, His) is the recombinant human-derived CD27/TNFRSF7 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of CD27/TNFRSF7 Protein, Human (Biotinylated, sf9, His) is 173 a.a., with molecular weight of ~20.7 kDa.
IL-13 Protein, Mouse is an immunoregulatory cytokine produced primarily by activated Th2 cells, and also by mast cells and NK cells. IL-13 exerts anti-inflammatory effects on monocytes and macrophages and it inhibits the expression of inflammatory cytokines such as IL-1β, TNF-α, IL-6 and IL-8.
The CD27/TNFRSF7 protein is a receptor for CD70/CD27L and may ensure the survival of activated T cells, suggesting that it plays a crucial role in immune responses. Its association with SIVA1 suggests a regulatory function in the apoptotic pathway. CD27/TNFRSF7 Protein, Human (Biotinylated, HEK293, Fc-Avi) is the recombinant human-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-Avi, C-hFc labeled tag. The total length of CD27/TNFRSF7 Protein, Human (Biotinylated, HEK293, Fc-Avi) is 173 a.a., with molecular weight of ~47.8 kDa.
IL-13 protein is a cytokine involved in allergic inflammation, immune response to parasites, and B cell proliferation. IL-13 Protein, Mouse (HEK293, His) is the recombinant mouse-derived IL-13 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of IL-13 Protein, Mouse (HEK293, His) is 110 a.a., with molecular weight of 14-30 kDa.
The CD27/TNFRSF7 protein is a receptor for CD70/CD27L and may ensure the survival of activated T cells, suggesting that it plays a crucial role in immune responses. Its association with SIVA1 suggests a regulatory function in the apoptotic pathway. CD27/TNFRSF7 Protein, Human (HEK293, His-Fc) is the recombinant human-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-hFc, C-6*His labeled tag. The total length of CD27/TNFRSF7 Protein, Human (HEK293, His-Fc) is 172 a.a., with molecular weight of ~60 kDa.
CD27/NFRSF7 Protein acts as a receptor for CD70/CD27L, supporting activated T-cell survival and potentially influencing apoptosis through interactions with SIVA1. It forms homodimers and engages with SIVA1 and TRAF2, indicating diverse roles in cellular processes. CD27/TNFRSF7 Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-hFc, C-6*His labeled tag. The total length of CD27/TNFRSF7 Protein, Mouse (HEK293, His-Fc) is 159 a.a., with molecular weight of 60-66 kDa.
CD27/TNFRSF7 Protein lacks conserved residue(s) crucial for feature annotation propagation, suggesting a unique structural characteristic. This peculiarity may influence CD27's functional properties within the TNFR superfamily, emphasizing the need for further investigation to understand its specific roles and regulatory mechanisms in cellular processes. CD27/TNFRSF7 Protein, Rhesus macaque (HEK293, Fc) is the recombinant Rhesus Macaque-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of CD27/TNFRSF7 Protein, Rhesus macaque (HEK293, Fc) is 172 a.a., with molecular weight of 60-75 kDa.
IL-13 protein is a cytokine involved in allergic inflammation, immune response to parasites, and B cell proliferation. Animal-Free IL-13 Protein, Mouse (His) is the recombinant mouse-derived animal-FreeIL-13 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free IL-13 Protein, Mouse (His) is 110 a.a., with molecular weight of ~13.06 kDa.
KBTBD8 in the BCR E3 ubiquitin ligase complex plays a critical regulatory role in neural crest specification. The BCR(KBTBD8) complex coordinates this action by monoubiquitinating NOLC1 and TCOF1. KBTBD8 Protein, Human (Sf9) is the recombinant human-derived KBTBD8 protein, expressed by Sf9 insect cells , with tag free. The total length of KBTBD8 Protein, Human (Sf9) is 600 a.a., .
KBTBD8 in the BCR E3 ubiquitin ligase complex plays a critical regulatory role in neural crest specification. The BCR(KBTBD8) complex coordinates this action by monoubiquitinating NOLC1 and TCOF1. KBTBD8 Protein, Human (Sf9, His, Strep) is the recombinant human-derived KBTBD8 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of KBTBD8 Protein, Human (Sf9, His, Strep) is 600 a.a., .
CD27/TNFRSF7 Protein lacks conserved residue(s) crucial for feature annotation propagation, suggesting a unique structural characteristic. This peculiarity may influence CD27's functional properties within the TNFR superfamily, emphasizing the need for further investigation to understand its specific roles and regulatory mechanisms in cellular processes. CD27/TNFRSF7 Protein, Rhesus macaque (HEK293, His) is the recombinant Rhesus Macaque-derived CD27/TNFRSF7 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CD27/TNFRSF7 Protein, Rhesus macaque (HEK293, His) is 172 a.a., with molecular weight of ~40.0 kDa.
The CD26/dipeptidyl peptidase 4 protein is a cell surface glycoprotein receptor that induces T cell proliferation and NF-kappa-B activation. CD26 also works with FAP to promote pericellular proteolysis, endothelial cell migration, and invasion of the extracellular matrix. CD26/Dipeptidyl Peptidase 4 Protein, Human (HEK293, His) is the recombinant human-derived CD26/Dipeptidyl Peptidase 4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CD26/Dipeptidyl Peptidase 4 Protein, Human (HEK293, His) is 738 a.a., with molecular weight of 86-130 kDa.
ICOS proteins play a critical role in enhancing all basic T cell responses to foreign antigens. It promotes cell proliferation, lymphokine secretion and upregulation of intercellular interaction molecules, and promotes effective B cell antibody secretion. ICOS Protein, Rhesus macaque (HEK293,Fc) is the recombinant Rhesus Macaque-derived ICOS protein, expressed by HEK293 , with C-hFc labeled tag. The total length of ICOS Protein, Rhesus macaque (HEK293,Fc) is 121 a.a., with molecular weight of 50-60 kDa.
The CD80 protein plays a key role in T lymphocyte activation, promoting proliferation and cytokine production through CD28 binding. In contrast, interaction with CTLA-4 inhibits T cell activation. CD80 Protein, Human (Cell-Free, His) is the recombinant human-derived CD80 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CD80 Protein, Human (Cell-Free, His) is 254 a.a., with molecular weight of 32.8 kDa.
B7-2/CD86 Protein, Mouse (HEK293, His), a second CTLA4 ligand expressed on murine B cells, can serve as a costimulatory molecule for T cell activation.
Linker for activation of T-cells Family Member 2; Linker for activation of B-cells; Membrane-Associated Adapter Molecule; Non-T-cellactivation Linker; Williams-Beuren Syndrome Chromosomal Region 15 Protein; Williams-Beuren Syndrome Chromosomal Region 5 Protei
NTAL protein is critical for FCER1 downstream signaling in mast cells and is involved in BCR-mediated signaling in B cells and FCGR1-mediated signaling in myeloid cells. It acts as a molecular bridge, recruiting GRB2 upon phosphorylation, linking receptor activation to intracellular responses. NTAL Protein, Human (HEK293, His) is the recombinant human-derived NTAL protein, expressed by HEK293 , with C-6*His labeled tag. The total length of NTAL Protein, Human (HEK293, His) is 217 a.a., with molecular weight of 35-40 kDa.
B7-H4 Protein, Human (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
B7-H4 Protein, Rhesus macaque (HEK293, His) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
B7-H4 Protein, Rhesus macaque (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
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 total length of VISTA/B7-H5 Protein, Mouse (159a.a, HEK293, His) is 159 a.a., with molecular weight of 30-40 kDa.
The B7-H4 protein acts as a negative regulator and inhibits T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. Significant significance can be observed when expressed on tumor macrophages, cooperating with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Mouse (sf9, His) is the recombinant mouse-derived B7-H4 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of B7-H4 Protein, Mouse (sf9, His) is 228 a.a., with molecular weight of ~26.6 kDa.
The B7-H4 protein acts as a negative regulator and inhibits T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. Significant significance can be observed when expressed on tumor macrophages, cooperating with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Mouse (HEK293, His) is 228 a.a., with molecular weight of ~26.6 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (HEK293, His) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Human (HEK293, His) is 230 a.a., with molecular weight of 43-48 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells (Tregs) to suppress tumor-associated antigen-specific T cell immunity and create an immunosuppressive microenvironment. B7-H4 Protein, Rat (HEK293, His) is the recombinant rat-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Rat (HEK293, His) is 228 a.a., with molecular weight of 42-65 kDa.
DNAM-1 protein is a key player in cell-cell adhesion and lymphocyte signaling, mediating cytotoxicity and lymphokine secretion of CTL and NK cells. As a receptor for NECTIN2, DNAM-1 stimulates T cell proliferation and cytokine production (IL2, IL5, IL10, IL13, and IFNG) upon ligand binding. DNAM-1 Protein, Human (HEK293, hFc, Myc) is the recombinant human-derived DNAM-1 protein, expressed by HEK293 , with C-Myc, C-hFc labeled tag. The total length of DNAM-1 Protein, Human (HEK293, hFc, Myc) is 229 a.a., with molecular weight of 56.1 kDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-His labeled tag. The total length of B7-H4 Protein, Human (Biotinylated, HEK293, His) is 230 a.a., with molecular weight of ~26.8 KDa.
The B7-H4 protein acts as a negative regulator, inhibiting T cell-mediated immune responses, including activation, proliferation, cytokine production, and cytotoxicity. When expressed on tumor macrophages, it cooperates with regulatory T cells to suppress tumor-associated antigen-specific T cell immunity. B7-H4 Protein, Human (Biotinylated, HEK293, Fc-Avi) is the recombinant human-derived B7-H4 protein, expressed by HEK293 , with C-Avi, C-hFc labeled tag. The total length of B7-H4 Protein, Human (Biotinylated, HEK293, Fc-Avi) is 230 a.a., with molecular weight of 70-95 kDa.
CD40L (CD154; TRAP) is a ligand to CD40/TNFRSF5, acts function by generating a costimulatory signal that up-regulates IL-4 synthesis. CD40L is specifically expressed on activated CD4+ T-lymphocytes and involves in activation of NF-κB/MAPK pathway. CD40L also involves in B cell differentiation, maturation, and apoptosis. CD40L in human, cleaved into 2 chains of membrane form (1-261 a.a.) and soluble form (113-261 a.a.) which serves as a ligand for integrins (ITGA5:ITGB1 and ITGAV:ITGB3). CD40L/CD154/TRAP Protein, Human (HEK293, hFc-Flag) has a total length of 248 amino acids (M13-L261), is expressed in HEK392 cells with N-terminal hFc- and Flag-tag.
CD40L/CD154/TRAP proteins stimulate T cell proliferation and cytokine production, acting as ligands for integrins and CD40 receptors to activate various cell-dependent effects such as B cell activation and NF-κ-B signaling. CD40L/CD154/TRAP Protein, Human (HEK293, N-hFc) is the recombinant human-derived CD40L/CD154/TRAP protein, expressed by HEK293 , with N-hFc labeled tag. The total length of CD40L/CD154/TRAP Protein, Human (HEK293, N-hFc) is 149 a.a., with molecular weight of ~49 kDa.
B7-H4 Protein, Mouse (HEK293, Fc) may participate in negative regulation of cell-mediated immunity in peripheral tissues. Cell-associated B7-H4 could also inhibit T cell response. B7-H4 acts as a morphogenic factor for cancer cells.
SH2D1A protein regulates receptors of the SLAM family (SLAMF1, CD244, LY9, CD84, SLAMF6, and SLAMF7). SH2D1A Protein, Human (His) is the recombinant human-derived SH2D1A protein, expressed by E. coli , with N-6*His labeled tag. The total length of SH2D1A Protein, Human (His) is 128 a.a., with molecular weight of ~16.0 kDa.
CD40L (CD154; TRAP) is a ligand to CD40/TNFRSF5, acts function by generating a costimulatory signal that up-regulates IL-4 synthesis. CD40L is specifically expressed on activated CD4+ T-lymphocytes and involves in activation of NF-κB/MAPK pathway. CD40L also involves in B cell differentiation, maturation, and apoptosis. CD40L in human, cleaved into 2 chains of membrane form (1-261 a.a.) and soluble form (113-261 a.a.) which serves as a ligand for integrins (ITGA5:ITGB1 and ITGAV:ITGB3). GMP CD40L/CD154/TRAP Protein, Human (HEK293) has a total length of 149 amino acids (M113-L261), is expressed in HEK392 cells under GMP standard with tag free.
4-Hydroperoxy Cyclophosphamide-d4 is the deuterium labeled 4-Hydroperoxy cyclophosphamide. 4-Hydroperoxy cyclophosphamide is the active metabolite form of the proagent Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces Tcell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders[1][2].
L-Kynurenine-13C10 (sulfate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive Tcell polarization to the anti-inflammatory Treg phenotype .
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat[1]. Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses Tcell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2[2][3][4][5].
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activatesautophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .