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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 activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity .
Belatacept (BMS 224818) is a selective T-cell costimulation blocker. Belatacept binds to CD 80/86 ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants .
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations .
Lenaldekar (LDK) inhibits human and murine T-cell expansiomn. Lenaldekar inhibits autoimmune T cell response. Lenaldekar also induces cancer cellapoptosis. Lenaldekar can be used for T-cell mediated autoimmune diseases research .
CTA056 is an ITK (IL-2-inducible T-cell kinase) inhibitor with an IC50 of 0.1 μM. CTA056 selectively targets malignant T cells and modulates oncomirs. CTA056 induces apoptosis and is a potential therapeutic agent for the research of T-cell leukemia and lymphoma .
LLO (91-99) (Listeriolysin O (91-99)), an exotoxin, is a class I MHC-restricted T-cell epitopes of listeriolysin (LLO). LLO (91-99) is an essential antigen for induction of T-cell mediated immunity in vivo .
HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity .
Pacanalotamab (AMG 420; BI-836909) is a bispecific T-cell engager (BiTE) targeting to BCMA and CD3ɛ. BCMA refers to B cell maturation antigen, as Pacanalotamab redirecting T cells to BCMA expressing cells on the cell surface. Pacanalotamab conducts T-cell redirected lysis of human multiple myeloma (MM) cell lines .
Heraclenin, a natural furanocoumarin, significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT) .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
Mogamulizumab (KW-0761) is a recombinant anti-CCR4 monoclonal antibody (MAb). Mogamulizumab can eliminate tumor cells by antibody-dependent cellular cytotoxicity (ADCC). Mogamulizumab can be used in the research of cancers, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL) .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
(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-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
(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-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma .
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability .
Hemagglutinin (48-68) is the 48-68 fragment of influenza virus hemagglutinin. Hemagglutinin (48-68) can induce proliferation of the peptide specific T-cell clones .
Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma .
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation .
(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-T cells, induces T-cell stimulatory responses in vitro (EC50=0.91 nM for TNF-α release) .
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 T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell lymphoma .
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity .
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 activates T-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 .
ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
Lulizumab pegol (BMS-931699) is an anti-CD28 antibody antagonist. Lulizumab pegol effectively inhibits T-cell proliferation and it can be used for the reseach of kidney transplantation and autoimmunity disease .
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values <10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation .
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values <10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation .
Benzosceptrin C is an inhibitor for PD-L1, which promotes programmed cell death ligand (PD-L1) degradation in a lysosomal pathway, enhances the cytotoxicity of T-cells and exhibits antitumor activity .
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment .
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-cell activation .
Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity .
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-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis .
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 .
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-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM .
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .
NJK14047 inhibits p38 MAPK and the differentation of naive T-cells to Th1 and Th17 cells. NJK14047 ameliorates the collage-induced rheumatoid arthritis and Imiquimod (HY-B0180)-induced psoriasis in mice .
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-cell activation .
Influenza Matrix Protein (61-72) is a peptide fragment derived from matrix protein of influenza viruses, corresponds to amino acids 61-72. Influenza Matrix Protein (61-72) is a specific epitope which can induce CD4 +T-cell response .
ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM .
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows high affinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease .
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. 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 T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation .
Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
LCMV GP (61-80) is a peptide fragment derived from lymphocytic choriomeningitis virus (LCMV) glycoprotein (GP), and corresponds to amino acids 61-80. LCMV GP (61-80) is a specific epitope which can induce CD4 +T-cell response .
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research .
Sydowimide A is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), T-cell protein tyrosine phosphatase (TCPTP) and leukocyte common antigen (CD45), with IC50 values of 1.5, 2.4 and 18.83 μM, respectively .
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
TJ191 is a potent and specific anti-cancer agent that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. TJ191 has no affects on the proliferation of other cancer cells or normal fibroblasts or immune cells. TJ191 can be used for cancer research .
Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
J9 is a small molecule that reverses Dexamethasone (HY-14648) resistance in T-cell acute lymphoblastic leukemia. J9 is lethal to CUTLL1 cells only in the presence of Dexamethasone. J9 inhibits CUTLL1 cell growth with an EC50 of 28 μM in combination with Dexamethasone .
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs) .
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20 + non-Hodgkin lymphomas (NHL) .
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 .
Tisagenlecleucel (CTL019) is an autologous anti-CD19 chimeric antigen receptor (CAR) T-cell therapy. Tisagenlecleucel targets and eliminates CD19-expressing B cells. Tisagenlecleucel can be used for the research of refractory aggressive diffuse large B-cell lymphoma .
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Abatacept (CTLA4lg) is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains) . Abatacept is a selective T-cell co-stimulation modulator and a protein agent for the autoimmune diseases .
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-cell activation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
Nivatrotamab (Hu3F8-BsAb) is a humanized anti-GD2/CD3 bispecific antibody. Nivatrotamab is a CD3- and GD2-specific bsAb-based T-cell engager. Nivatrotamab can be used in research of neuroblastoma .
Anti-DLL3 Antibody (anti-DLL3 arm derived from AMG-757) is the anti-DLL3 arm of the bispecific T-cell engager (BiTE) antibody-Tarlatamab (AMG-757) (HY-P99575). Tarlatamab targets both DLL3 and CD3.
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 activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC) .
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research .
PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
Abatacept (CTLA4lg; BMS-188667) powder is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains). Abatacept powder is a selective T-cell co-stimulation modulator and a protein agent for the autoimmune diseases .
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 T cell activation or toxicity .
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 .
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cellsin vitro and in vivo .
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
Surzebiclimab (BGB-A425) is a humanized IgG1-variant monoclonal antibody against T-cell immunoglobulin and mucin-domain containing-3 (TIM-3). Surzebiclimab binds to the extracellular domain of human Tim-3 with high affinity (KD=0.36 nM) and specificity. Surzebiclimab can be used in research of cancer .
Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
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-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al .
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases .
Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer .
JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for autoimmune disease research .
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection .
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) .
1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay .
PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research .
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (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 .
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-κB activation 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 .
Sintilimab (IBI308) is a fully human IgG4 monoclonal antibody that binds to PD-1, thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2) and consequently helping to restore the endogenous antitumour T-cell response. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
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-activated T-lymphocytes respectively). KV1.3-IN-1 impairs intracellular Ca 2+ signaling. KV1.3-IN-1 inhibits T-cell activation, proliferation, and colony formation .
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes T cells, decreases T cell activation, inhibites T cell proliferation and enriches naïve and bona fide regulatory T cells .
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research .
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-cell activation - .
LSD1/2-IN-4, a PCPA derivative, is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with Ki values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL) .
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels .
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs .
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-cell activation - .
Immune cell migration-IN-2 is a potent immune cell migration inhibitor with an EC50 of 13.5 nM in a T-cell adhesion assay. Immune cell migration-IN-2 is extracted from patent WO2019001171, example 11, can be used for dry-eye and other retinal diseases research . Immune cell migration-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
TIM-3-IN-2 (Compound A-41) is a Tim3 inhibitor (KD: 0.61 μM). TIM-3-IN-2 blocks TIM-3 interactions with PtdSer, CEACAM1, and Gal-9. TIM-3-IN-2 inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 reverses the TIM-3-mediated blockade of the production of proinflammatory cytokines, and maximizes the T-cell antitumor activity against AML cell lines .
Peptide A5K (INF7-A5K-TAT) is an RNP delivery peptide that delivers CRISPR RNPs to T cells. Peptide A5K effectively edits T cells without substantial impact on T cell viability .
Teclistamab is a human bispecific antibody to BCMA and CD3 that recognizes BCMA on target cells and CD3 on T cells and induces T cell-mediated cytotoxicity leading to T cell activation and subsequent target cell lysis. Teclistamab can be used in studies of diseases related to multiple myeloma (MM) .
PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
Cibisatamab (CEA-TCB), a T cell bispecific antibody, binds Carcino-Embryonic Antigen (CEA) on cancer cells and CD3 on T cells. Cibisatamab (CEA-TCB) triggers T cell killing of cancer cell lines expressing moderate to high levels of CEA at the cell surface. Cibisatamab (CEA-TCB) can be used for colorectal cancer research .
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation[1][2].
Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation .
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65) specific agonist. BTB09089 increases TDAG8 expression and regulates the cytokine production of T cells and macrophages .
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 .
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 T cells and can induce T cell stimulation in vitro (EC50=0.39 nM, TNF-α) .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) .
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile .
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on T cells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces T cell activation and proliferation .
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 T cell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8 +T cells and reduces T cell exhaustion .
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 +T cells into other lineages, including Th1 and regulatory T cells .
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling .
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 T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to T cells. Phospholipid PL1 could induce the activation of various immune cells, including T cells and dendritic cells (DCs) in order to boost antitumor immunity .
Tebotelimab (MGD-013) is a humanized IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity .
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development .
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively .
Cevostamab (BFCR4350A; RG6160; RO7187797) is a humanized IgG1-based BsAb that targets membrane-proximal extracellular domain of FcRH5 on multiple myeloma (MM) cells as well as CD3 on T cells. Moreover, Cevostamab facilitates efficient synapse formation, improves killing activity of T cells against MM tumor cells .
(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell 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 .
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 T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cellApoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM .
Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment .
Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease .
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT .
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
Tepoditamab (MCLA-117) is a bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab (MCLA-117) kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells and can be used in acute myeloid leukaemia (AML) research .
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype .
LTV-1 is a potent lymphoid tyrosine phosphatase (LYP) inhibitor in T cells with an IC50 of 508 nM. LTV-1 has the potential for autoimmunity treatment .
AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells .
CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist . RBD: receptor-binding domain
Gotistobart (ONC-392) is a humanized anti-CTLA-4 antibody that confers immunotherapeutic effect by selective depletion of regulatory T cells (Treg) in the tumor microenvironment .
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 T cell Activation .
Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .
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 T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells .
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
11R-VIVIT is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT can be used for the research of podocyte and diabetic nephropathy .
Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
Necrostatin 2 is also a RIPK1 inhibitor.
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3 .
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 T cell activation and increases IL-2 production in primary human T Cells .
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis .
CI 972 anhydrous is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (Ki=0.83 μM) under development as a T cell-selective immunosuppressive agent .
11R-VIVIT TFA is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy .
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
Muromonab is a monoclonal antibody targeting the CD3 receptor. Muromonab can block all cytotoxic T cell function. Muromonab also as an immunosuppressant agent given to reduce acute solid organ transplant rejection .
ITF 3756 is a potent and selective HDAC6 inhibitor. ITF 3756 reduces in vitro the expression of PD-L1 on human monocytes and on CD8 T cells, and shows anti-tumor activity .
Sulfamethoxazole-NO (SMX-NO) hydrate is the reactive metabolite of SMX (HY-B0322). Sulfamethoxazole-NO (SMX-NO) hydrate actis as a typical hapten and is capable of covalently modifying the MHC-peptide complex, can stimulate hapten-reactive T cells .
Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells .
Vabametkib is a potent inhibitor of hepatocyte growth factor receptor (HGFR). Vabametkib inhibits Hs746T cells proliferation and inhibits c-Met with an IC50 value of 7 nM. Vabametkib can be used as an antineoplastic agent .
P-2281 is a mTOR inhibitor with anticancer and anti-inflammatory efficacies. P-2281 suppresses dextran sulfate sodium (DSS)-induced colitis by inhibiting T cell function and is efficacious in a murine model of human colitis .
Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 +T cells.
Ipilimumab is a fully human monoclonal antibody IgG1κ that blocks the inhibitory receptor cytotoxic T lymphocyte antigen 4 (CTLA-4) on T cells. Ipilimumab can be used in unresectable or metastatic melanoma (MM) studies .
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 - .
Tulipalin A (α-Methylene butyrolactone) is a glycoside. Tulipalin A is a causative allergen that induces Allergic contact dermatitides . Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells .
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease .
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
Tivumecirnon (FLX475) is an orally active CCR4 antagonist that blocks regulatory T cells from entering the tumor microenvironment, thereby reducing their interference with effective anti-tumor immune responses. Tivumecirnon has antitumor activity .
JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a Ki value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation .
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis .
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 T cell activation and antitumor immunity .
C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides . C6 L-threo Ceramide significantly inhibits IL-4 production in T cells. Anti-allergic agents .
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer .
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 T cell subsets and T regulatory cells .
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 activated T cells toward CXCL11 .
Prostaglandin B2 is a prostaglandin. Prostaglandin B2 is the main substance in cord blood mesenchymal stem cells, to inhibit DC-T Cell proliferation. Prostaglandin B2 also induces cutaneous vasoconstriction of the canine hind paw .
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively .
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases .
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
Theralizumab (TGN1412) is a humanized lgG4 superagonistic anti-CD28 monoclonal antibody that directly stimulates T cells. Theralizumab can cause cytokine release syndrome (CRS). Theralizumab can be used for the research of rheumatoid arthritis .
NC1 is a noncompetitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 inhibits LYP by restricting the movement of the WPD-loop. NC1 inhibits LYP-mediated TCR signaling in T cells .
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activated T cells, NK cells, B cells and plasmacytoid dendritic cells .
Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl proagent of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 +T cells.
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases .
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM .
L-Kynurenine- 13C10 (sulfate hemihydrate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate hemihydrate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Tebuconazole (Standard) is the analytical standard of Tebuconazole. This product is intended for research and analytical applications. Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells .
Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil . Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat .
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent .
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM . Psora-4 has immunosuppressive activity and inhibits proliferation of human and rat myelin-specific effector memory T cells in vitro .
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 T cell activation .
Vibecotamab (XmAb14045) is a potent bispecific antibody against CD123 and CD3 that stimulates T cell-mediated targeted killing of CD123-expressing cells. Vibecotamab has antitumor activity and can be used in acute myeloid leukaemia studies .
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 T cells. Nemvaleukin alfa can be used for research of cancer .
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ T cell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase . Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity .
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase . Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity .
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS) .
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (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 T cells and the haemocyte non-self response in Lepidoptera larve .
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
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 T cell polarization to the anti-inflammatory Treg phenotype .
P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia .
SP-2-225 is a selective HDAC6 inhibitor. SP-2-225 enhance the production of cancer-associated antigens and macrophage antigen cross-presentation to T cells. SP-2-225 reduces the tumor volume in a syngeneic SM1 melanoma model .
DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor. DGKα&ζ-IN-1 can enhance the function of T cells, and has a synergistic effect with PD-1, which has therapeutic effects IN both immune and tumor .
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
Caerin 1.1 TFA is a host defense peptide isolated from the glandular secretions of the Australian tree frog Litoria. Caerin 1.1 TFA inhibits HeLa cell proliferation and mediates apoptosis. Caerin 1.1 TFA may enhance adaptive T cell immune responses .
ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1.
ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .
GSK-5498A is a selective CARC channel inhibitor (IC50: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders .
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function .
Keliximab (SB-210396) is a chimeric human/macaque IgG1 anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research .
LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model .
Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cellsapoptosis .
UU-T01 is a selective inhibitor for β-Catenin/T-cell factor 4 protein-protein interaction (β-catenin/Tcf PPI) with an Ki value of 3.14 µM. UU-T01 is directly combined with β-catenin, and the KD value is 0.531 µM .
LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research .
Semzuvolimab is a murine IgG1κ antibody, targeting to p55, T cell surface antigen T4/Leu-3 (CD4). Murine CD4 antibodies can neutralize HIV infection and have the potential to inhibit HAART stable HIV infection .
GAD65(247-266) epitope TFA is the T cell epitopes of islet antigens,binding to I-A g7 (type I diabetes-associated molecule) competitively with poor affinity. GAD65 refers to Glutamic Acid Decarboxylase 65,involved in the conversion of glutamate to gamma-aminobutyric acid (GABA) .
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat[1]. Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2[2][3][4][5].
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 T cell infiltration and activation .
9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively .
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells .
PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment .
UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) with a Ki of 1.36 μM . UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells .
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus .
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo .
JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6 nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions .
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model .
Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor) .
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment .
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity .
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 +T cell activation. 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 HEK293T cells (IC50= 89 nM) .
TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice .
CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .
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 T cell activation by inhibiting IL-2 expression .
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 research. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer .
SRI-37240 is a potent premature termination codons (PTCs) inhibitor. SRI-37240 suppresses CFTR nonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restore CFTR function in primary bronchial epithelial cells when combination with G418 .
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 T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .
Pristane-d40 is the deuterium labeled Pristane[1]. Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil[2]. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat[3].
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity .
4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce T cell 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 .
β-catenin-IN-37 is a selective β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) inhibitor. β-catenin-IN-37 inhibits canonical Wnt signaling and the growth of colorectal cancer cellsSW480 and HCT116 with the IC50 values of 20 μM and 31 μM, respectively .
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
Purine nucleoside phosphorylase, Microorganism (PNP) is a key enzyme in purine metabolism, which is involved in the purine rescue pathway. The deficiency of Purine nucleoside phosphorylase resulted in impaired T cell function. In the presence of inorganic orthophosphate as the second substrate, Purine nucleoside phosphorylase catalyzes the breaking of the glycosidic bond between ribose and deoxyribonucleoside to generate purine base and ribose (deoxyribose) -1-phosphate .
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC50 of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC50 of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
DGKα-IN-4 (example 432) is a DGKα inhibitor with the IC50 of 0.1 nM, extracted from patent WO2021105117. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-3 has the potential for cancer and immunology study.
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 +T cell activation. RDN2150 TFA can be used for research of psoriasis .
Rp-dGTPαS is the nucleotide substrate of SAMHD1 and is one of the enantiomers of the dNTPαS nucleotide. SAMHD1 is an essential regulator of cellular dNTPs that limits virus (HIV-1, etc.) replication in the CD4+ myeloid lineage and resting T cells. The SAMHD1 tetrameric complex catalyzes the hydrolysis of Rp-dGTPαS into 2'-deoxynucleosides and triphosphates .
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis .
RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23) .
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17) .
Toralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab, a immunosuppressive agent, has the potential for active systemic lupus erythematosus (SLE) research .
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) .
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 T cell activation and amplifies IFN-γ-mediated cytotoxicity. PVD-06 has anticancer activity .
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
SIRT6-IN-2 (Compound 5) is a selective SIRT6 inhibitor (IC50: 34 μM). SIRT6-IN-2 increases acetylation of H3K9 and increases glucose uptake in cultured cells. SIRT6-IN-2 also reduces T cell proliferation. SIRT6-IN-2 has immunosuppressive and chemosensitizing effects .
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
Z36-MP5 is an Mi-2β-targeted inhibitor, with IC50 of 0.082 μM. Z36-MP5 can reduce Mi-2β ATPase activity and reactivates ISG transcription. Z36-MP5 can stimulate T-cell-mediated cytotoxicity .
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively . Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases .
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression .
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 T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation . YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma .
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs .
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .
Trehalose 6,6'-dimycolate (Cord Factor) is trehalose 6,6'-dimycolate, a cell wall glycolipid of Mycobacterium tuberculosis, which can be used to simulate inflammation and granuloma induced by Mycobacterium tuberculosis (MTB) form. Trehalose 6,6′-dimycolate also protects Mycobacterium tuberculosis from macrophage-mediated killing, inhibits efficient antigen presentation, and reduces the development of protective T cell responses .
Eciskafusp alfa is a programmed cell death 1 (PDCD1, best known as PD-1) cis-targeted IL2v immunocytokine. Eciskafusp alfa preferentially targets antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells and differentiates them towards a novel population of better effectors. Eciskafusp alfa can be used for the research of cancer and chronic infections .
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 T cell activation .
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 T cell activation .
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
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 +T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. 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 .
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
LSD1-IN-27 (Compound 5ac) is a LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer .
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus .
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation 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 T cell activation 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.
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 T cell 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].
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells .
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 T cells. 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), T cells 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), T cells 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) .
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases .
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
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 T cells efficiently in PBMCs. PD-1/PD-L1-IN-25 can be used for the research of cancer .
HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs) .
Latikafusp (AMG 256) is a bifunctional fusion protein comprising a PD-1-targeting antibody and IL-21 mutein designed to deliver IL-21 pathway stimulation to PD-1+ cells. Latikafusp is designed to prime and extend the activity of cytotoxic and memory T cells and induce anti-tumor immunity. Latikafusp has the potential for solid tumors research .Latikafusp may lead to the development of immunogenicity-mediated responses .
CD19 CAR mRNA will express CD19 car protein, and can be used in chimeric antigen receptor T cell 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 T cell 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.
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) .
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell 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 .
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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+ T cell activation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth .
PD-1/ PD-L1-in-38 is a PD-1/PD-L1 inhibitor, which can inhibit the proliferation of tumor cells, promote the secretion of INF-γ by CD8 +T cells, and inhibit the ability of PD-1/PD-L1 signal transduction. PD-1/PD-L1-IN-38 has antitumor activity .
Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
AS2863619 enables conversion of antigen-specific effector/memory T cells 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. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
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 T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4 +T cells and CD11b + macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA . Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM .
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 T cells activation 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 .
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 activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
Ferrichrome is a hydroxamate siderophore produced by various fungi, including U. sphaerogena, that facilitates iron chelation and uptake by these organisms. It can be used as a heterosiderophore by bacteria, including Pseudomonas aeruginosa and Vibrio parahaemolyticus. Ferrichrome (0.8 μM) inhibits concanavalin A-induced proliferation of mouse spleen monocytes and reduces the number of concanavalin A-stimulated CD4+ T cells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies . SS47 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Reltecimod (AB-103) TFA is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod TFA has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod TFA modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod TFA can be used to research necrotizing soft-tissue infections (NSTIs) .
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 T cell activation and can be used in cancer immunity research .
3,4-DAA is an orally active Anthranilic acid derivative with potent immunosuppressive activities. 3, 4-DAA can alleviate the severity of colitis through inhibiting Th1 cells response, promoting Th2 cytokines expression and inducing CD4 +CD25 +T cells expression . 3,4-DAA suppressed expression of inducible nitric oxide synthase (iNOS) and nitric oxide (NO) release from EOC20 cells induced by IFN-γ and Lipopolysaccharide .
A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death .
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
AS2863619 free base enables conversion of antigen-specific effector/memory T cells 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. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene .
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases .
(2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8 +T cells and inhibits the signal transduction of PD-1/PD-L1 .
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 T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1) .
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
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 T cells 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 T cell activation .
Incomplete Freund's adjuvant (IFA) (Montanide ISA-51) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund. Incomplete Freund's adjuvant (IFA) does not contain inactivated tuberculosis bacilli and consists of petroleum jelly containing lanolin. Incomplete Freund's adjuvant (IFA) induces high antibody titers and long-lasting effector T cell responses with no long-term effects on collagen disease, tumors, or death. Complete Freund's adjuvant (CFA) (HY-153808) is another type of Freund's Adjuvant that stimulates a stronger immune response .
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 cell activation and promotes the proliferation of CD4 + T and CD8 +T cells, 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 .
Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity .
(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 T cells .
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 T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
Ssm Spooky Toxin from?Scolopendra mutilans, exhibits lethal toxicity in hematological and respiratory systems by potently inhibiting KCNQ (voltage-gated potassium channel family 7) channels, with IC50? of 2.8 μM, 5.26 μM and 0.1-0.3 M for Kv7.4, Kv1.3, and Shal channel, respectivily. Ssm Spooky Toxin inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin plays an essential role in the centipede’s circulatory system .
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 +T cells .
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 T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
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 T cell 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 T cell 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 .
PD-L1-IN-3 (Compound 4a) is a compound that targets PD-1/PD-L1, the IC50 value and EC50 value is 4.97nM and 2.70 μM for inhibit PD-L1 and Jurkat T cells, respectively. PD-L1-IN-3 can bind PD-L1 dimer to prevent PD-1 binding to PD-L1, therefore blocking PD-1 signaling. PD-L1-IN-3 can be used for lung cancer and melanoma diseases research .
(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) cell activation and tumor targeting .
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 +T cells .
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 T cell activation .
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 T cells .
Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer .
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
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 T cell activation. 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-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to T cells. Phospholipid PL1 could induce the activation of various immune cells, including T cells and dendritic cells (DCs) in order to boost antitumor immunity .
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis .
Trehalose 6,6'-dimycolate (Cord Factor) is trehalose 6,6'-dimycolate, a cell wall glycolipid of Mycobacterium tuberculosis, which can be used to simulate inflammation and granuloma induced by Mycobacterium tuberculosis (MTB) form. Trehalose 6,6′-dimycolate also protects Mycobacterium tuberculosis from macrophage-mediated killing, inhibits efficient antigen presentation, and reduces the development of protective T cell responses .
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 T cell 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 T cell 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 .
TET 830 modified/T-helper epitope from tetanus toxoid is a modified T-helper epitope from tetanus toxoid. TET 830 modified/T-helper epitope from tetanus toxoid induces T-cells responses and is used as a helper peptide in vaccinations .
LLO (91-99) (Listeriolysin O (91-99)), an exotoxin, is a class I MHC-restricted T-cell epitopes of listeriolysin (LLO). LLO (91-99) is an essential antigen for induction of T-cell mediated immunity in vivo .
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)
Tiplimotide (NBI-5788) is an altered peptide ligand (APL) designed from an immunodominant region (83-99) of the neuroantigen myelin basic protein (MBP). Tiplimotide can selectively reduce the production of inflammatory cytokines by pathogenic T-cells. Tiplimotide can be used for the research of multiple sclerosis (MS) .
Hemagglutinin (48-68) is the 48-68 fragment of influenza virus hemagglutinin. Hemagglutinin (48-68) can induce proliferation of the peptide specific T-cell clones .
AAV2 Epitope is a biological active peptide. (This peptide is the capsid derived immunodominant adeno-associated virus 2 (AAV2), CD8 T cell epitope. Liver toxicity observed in a clinical trial of AAV2 delivered systemically to patients with hemophilia was ascribed to killing of vector-transduced hepatocytes by capsid-specific T-cells.)
MOG peptide (35-55) is a fragment 35-55 of myelin oligodendrocyte glycoprotein (MOG) immunogenic peptide. MOG peptide (35-55) is specific to expanded CD4 +T cells, and induces experimental autoimmune encephalomyelitis (EAE) in animal model .
Influenza Matrix Protein (61-72) is a peptide fragment derived from matrix protein of influenza viruses, corresponds to amino acids 61-72. Influenza Matrix Protein (61-72) is a specific epitope which can induce CD4 +T-cell response .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
LCMV GP (61-80) is a peptide fragment derived from lymphocytic choriomeningitis virus (LCMV) glycoprotein (GP), and corresponds to amino acids 61-80. LCMV GP (61-80) is a specific epitope which can induce CD4 +T-cell response .
NY-BR-1 p904 (A2) is an HLA-A2-restricted NY-BR-1 epitope. T-cell clone specific for NY-BR-1 p904 can recognize breast tumor cells expressing NY-BR-1 .
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
CMV pp65(13-27) is a biological active peptide. (This peptide is derived from amino acid residues 13 to 27 of the 65k lower matrix phosphoprotein of the human cytomegalovirus. It contains a nine-amino-acid sequence (LGPISGHVL) that matches the consensus binding motif for a major histocompatibility complex H2-Dd T-cell epitope.)
NY-ESO-1 (87-111) is a pan-MHC class II-restricted peptide sequence. NY-ESO-1 (87-111) binds to multiple HLA-DR and HLA-DP4 molecules, and stimulates Th1-type and Th-2/Th0-type CD4 +T cells when presented in the context of HLA-DR and HLA-DP4 molecules .
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
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-cell activation - .
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-cell activation - .
Peptide A5K (INF7-A5K-TAT) is an RNP delivery peptide that delivers CRISPR RNPs to T cells. Peptide A5K effectively edits T cells without substantial impact on T cell viability .
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 T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
BDC2.5 mimotope 1040-31, a BDC2.5 TCR reactive peptide, is a strong agonistic peptide for diabetogenic T cell clone BDC2.5, and the 1040-31 peptide is specific for BDC 2.5 TCR Tg + T cells .
BDC2.5 mimotope 1040-31 TFA, a BDC2.5 TCR reactive peptide, is a strong agonistic peptide for diabetogenic T cell clone BDC2.5, and the 1040-31 peptide is specific for BDC 2.5 TCR Tg + T cells .
Binetrakin (Interleukin 4 (human)) is a T lymphocyte-derived pleiotrophic cytokine that affects a variety of cell types including B cells and T cells. Binetrakin induces differentiation of naive helper T cells (Th0 cells) to Th2 cells. Binetrakin can be used for the research of many biological .
BDC2.5 Mimotope 1040-63 is a biological active peptide. (The TCR transgenic model (BDC2.5) mimitope was used in type 1 diabetes (T1D) study. T1D is an autoimmune disease in which T cells mediate damage to pancreatic islet b cells. T1D is caused by autoreactive T cell destruction of insulin-producing cells. BDC2.5 mimotope was utilized to support the study on antigen presentation of antigenic peptides to islet autoantigen-specific T cells.)
GAD65 (206-220) is glutamic acid decarboxylase (GAD) 65-derived peptide, corresponding to residues 180-188. GAD65 is presented to T cells in association with I-Ag7 MHC class II molecules and a major pancreatic antigens targeted by self-reactive T cells in type I diabetes mellitus .
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
Cytochrome c-pigeon (88-104) (PCC 88-104) has full stimulatory activity for pigeon cytochrome c-primed T cells from B10.A mice. The I-E k-restricted T cell response to Cytochrome c pigeon (pcyt c) is specific for the COOH-terminal sequence 88-104 .
Influenza NP (311-325) is a biological active peptide. (This peptide is amino acids 311 to 325 fragment of the influenza virus nucleoprotein (NP). This bona fide MHC class II restricted epitope from influenza virus was used to study the host immunoresponse during the infection. This peptide elicits the strongest gamma interferon (IFN-gamma) production in the intracellular cytokine assays. It does not stimulate CD8 T-cells in mice.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT .
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 T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells .
11R-VIVIT is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT can be used for the research of podocyte and diabetic nephropathy .
11R-VIVIT TFA is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy .
OVA G4 peptide is a variant of the agonist ovalbumin (OVA) peptide SIINFEKL (257-264). SIINFEKL is routinely used to stimulate ovalbumin-specific T cells and to test new vaccine adjuvants can form a stable hydrogel .
OVA G4 peptide TFA is a variant of the agonist ovalbumin (OVA) peptide SIINFEKL (257-264). SIINFEKL is routinely used to stimulate ovalbumin-specific T cells and to test new vaccine adjuvants can form a stable hydrogel .
YLLEMLWRL is an HLA-A2-restricted T cell epitope sequence corresponding to codon 125-133. Among them, YLLEMLWRL sequence is the main mutation site of HLA-A2-restricted CTL epitope sequence .
Gp100 (25-33), human (Hgp100 (25-33)) is the amino acids 25-33 fragment of the human melanoma antigen. It is a 9-amino acid (AA) epitope restricted by H-2D b and recognized by the T cells .
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases .
VLHDDLLEA is a peptide that can be isolated from the MHC complex HLA-A*0201 molecule. VLHDDLLEA can be recognized by HLA-A*0201-restricted cytotoxic T cells (CTLs). VLHDDLLEA can be used for research on graft versus host disease (GvHD) .
Tyrosinase (192-200), human mouse is a nonapeptide. Tyrosinase (192-200), human mouse can be recognized by cytolytic T cell (CTL) on the HLA-B44 molecule. Tyrosinase (192-200), human mouse can be used in research of melanoma associated cancers .
CFP10 (71–85) is a biological active peptide. (CFP1071–85, that elicited IFN-γ production and CTL activity by both CD4+ and CD8+ T cells from persons expressing multiple MHC class II and class I molecules)
Gp100 (25-33), human TFA (Hgp100 (25-33) TFA) is the amino acids 25-33 fragment of the human melanoma antigen. It is a 9-amino acid (AA) epitope restricted by H-2D b and recognized by the T cells .
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
Myelin Basic Protein(87-99) TFA is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) TFA causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS) .
Caerin 1.1 TFA is a host defense peptide isolated from the glandular secretions of the Australian tree frog Litoria. Caerin 1.1 TFA inhibits HeLa cell proliferation and mediates apoptosis. Caerin 1.1 TFA may enhance adaptive T cell immune responses .
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function .
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)
Peripheral Myelin Protein P2 (53-78), bovine is derived from bovine peripheral myelin P2 protein amino acid residues 53-78. Peripheral Myelin Protein P2 (53-78), bovine is a T cell epitope for the induction of experimental autoimmune neuritis (EAN) in Lewis rats .
GAD65(247-266) epitope TFA is the T cell epitopes of islet antigens,binding to I-A g7 (type I diabetes-associated molecule) competitively with poor affinity. GAD65 refers to Glutamic Acid Decarboxylase 65,involved in the conversion of glutamate to gamma-aminobutyric acid (GABA) .
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus .
Peptide A5K (INF7-A5K-TAT acetate) acetate is a INF7-TAT derivative and is used for CRISPR RNP delivery into T cells. Peptide A5K acetate effectively promotes the delivery of Cas9 RNP to natural killer (NK) cells .
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 HEK293T cells (IC50= 89 nM) .
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
Des-[Gly77,His78] Myelin Basic Protein (68-84) is a 68-84 sequence fragment of guinea pig myelin basic protein (GPMBP). Des-[Gly77,His78] Myelin Basic Protein (68-84) regulates functionally diverse encephalitogenic and proliferative activities of experimental autoimmune encephalomyelitis (EAE)-associated T cells .
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs .
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs) .
β-Interleukin I (163-171), human, an immunostimulatory fragment of human IL-1β peptide, is a T cell activator. 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 T cell-mediated autoimmune diseases .
Hyaluronan-binding peptide, biotin labeled is a biological active peptide. (This peptide is a hyaluronan-binding peptide biotinylated through a C-terminal GGGSK linker. Hyaluronan (HA) is a nonsulfated glycosaminoglycan expressed in the extracellular matrix and on cell surfaces. HA plays a role in fertilization, embryonic development, wound healing, angiogenesis, leukocyte trafficking to inflamed tissues, and cancer metastasis. This peptide has been shown to block HA binding to CD44 receptors and inhibit T cell proliferation.)
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell 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 .
Ferrichrome is a hydroxamate siderophore produced by various fungi, including U. sphaerogena, that facilitates iron chelation and uptake by these organisms. It can be used as a heterosiderophore by bacteria, including Pseudomonas aeruginosa and Vibrio parahaemolyticus. Ferrichrome (0.8 μM) inhibits concanavalin A-induced proliferation of mouse spleen monocytes and reduces the number of concanavalin A-stimulated CD4+ T cells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
Reltecimod (AB-103) TFA is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod TFA has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod TFA modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod TFA can be used to research necrotizing soft-tissue infections (NSTIs) .
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) acetate is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) TFA is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
Ssm Spooky Toxin from?Scolopendra mutilans, exhibits lethal toxicity in hematological and respiratory systems by potently inhibiting KCNQ (voltage-gated potassium channel family 7) channels, with IC50? of 2.8 μM, 5.26 μM and 0.1-0.3 M for Kv7.4, Kv1.3, and Shal channel, respectivily. Ssm Spooky Toxin inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin plays an essential role in the centipede’s circulatory system .
MCE Mouse CD3+T Cells Negative Selection Kit is designed for the isolation of CD3+T cells from single cell suspensions of mouse spleen cells, lymph nodes or other tissues.
MCE Mouse CD4+T Cells Negative Selection Kit is designed for the isolation of CD4+T cells from single cell suspensions of mouse spleen cells, lymph nodes or other tissues.
MCE Mouse CD8+T Cells Negative Selection Kit is designed for the isolation of CD8+T cells from single cell suspensions of mouse spleen cells, lymph nodes or other tissues.
MCE Mouse CD4+T Cells Positive Selection Kit is designed for the isolation of CD4+cells from single cell suspensions of mouse spleen cells, lymph nodes or other tissues.
Tinurilimab (Bay 1834942) is an anti-CEACAM6 monoclonal antibody. CEACAM6 is an immune checkpoint regulator suppressing the activity of effector T-cells against tumors .
Pacanalotamab (AMG 420; BI-836909) is a bispecific T-cell engager (BiTE) targeting to BCMA and CD3ɛ. BCMA refers to B cell maturation antigen, as Pacanalotamab redirecting T cells to BCMA expressing cells on the cell surface. Pacanalotamab conducts T-cell redirected lysis of human multiple myeloma (MM) cell lines .
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
Zanolimumab (Anti-Human CD4 Recombinant Antibody) is a fully human monoclonal antibody targets CD4. Zanolimumab effectively inhibits T-cell receptor (TCR) signal transduction. Zanolimumab can be used for the research of heumatoid arthritis, psoriasis, melanoma, cutaneous and peripheral T-cell lymphoma .
Mogamulizumab (KW-0761) is a recombinant anti-CCR4 monoclonal antibody (MAb). Mogamulizumab can eliminate tumor cells by antibody-dependent cellular cytotoxicity (ADCC). Mogamulizumab can be used in the research of cancers, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL) .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
Tamgiblimab (IBI939) is a fully human monoclonal antibody targeting T-cell immunoreceptor with immunoglobulin and ITIM domains (TIGIT). Tamgiblimab has anticancer effects .
Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma .
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 T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell lymphoma .
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity .
Lulizumab pegol (BMS-931699) is an anti-CD28 antibody antagonist. Lulizumab pegol effectively inhibits T-cell proliferation and it can be used for the reseach of kidney transplantation and autoimmunity disease .
Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment .
Lacutamab (IPH4102) is a humanizedized monoclonal antibody (mAb) directed against the immune receptor molecule KIR3DL2, produced by recombinant technology in CHO cells. Lacutamab can be used in research of cutaneous T-cell lymphoma .
Tamtuvetmab (AT-005) is a caninised blontuvetmab against CD52. Tamtuvetmab increases progression-free survival (PFS), exhibits in vivo efficacy in dogs with naïve T-cell lymphoma (LSA). Tamtuvetmab has been approved by veterinary .
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 .
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-cell activation .
Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20 + non-Hodgkin lymphomas (NHL) .
Tisagenlecleucel (CTL019) is an autologous anti-CD19 chimeric antigen receptor (CAR) T-cell therapy. Tisagenlecleucel targets and eliminates CD19-expressing B cells. Tisagenlecleucel can be used for the research of refractory aggressive diffuse large B-cell lymphoma .
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
Abatacept (CTLA4lg) is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains) . Abatacept is a selective T-cell co-stimulation modulator and a protein agent for the autoimmune diseases .
Tiragolumab is an immune checkpoint inhibitor binding to T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab, alone or in combination with the PD-L1 inhibitor Atezolizumab (HY-P9904), may be effective against multiple solid malignancies-most notably non-small cell lung cancer (NSCLC) .
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-cell activation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
Nivatrotamab (Hu3F8-BsAb) is a humanized anti-GD2/CD3 bispecific antibody. Nivatrotamab is a CD3- and GD2-specific bsAb-based T-cell engager. Nivatrotamab can be used in research of neuroblastoma .
Anti-DLL3 Antibody (anti-DLL3 arm derived from AMG-757) is the anti-DLL3 arm of the bispecific T-cell engager (BiTE) antibody-Tarlatamab (AMG-757) (HY-P99575). Tarlatamab targets both DLL3 and CD3.
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC) .
Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research .
Abatacept (CTLA4lg; BMS-188667) powder is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains). Abatacept powder is a selective T-cell co-stimulation modulator and a protein agent for the autoimmune diseases .
Surzebiclimab (BGB-A425) is a humanized IgG1-variant monoclonal antibody against T-cell immunoglobulin and mucin-domain containing-3 (TIM-3). Surzebiclimab binds to the extracellular domain of human Tim-3 with high affinity (KD=0.36 nM) and specificity. Surzebiclimab can be used in research of cancer .
Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer .
Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab (HY-P9913). Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL) .
Sintilimab (IBI308) is a fully human IgG4 monoclonal antibody that binds to PD-1, thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2) and consequently helping to restore the endogenous antitumour T-cell response. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes T cells, decreases T cell activation, inhibites T cell proliferation and enriches naïve and bona fide regulatory T cells .
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research .
Teclistamab is a human bispecific antibody to BCMA and CD3 that recognizes BCMA on target cells and CD3 on T cells and induces T cell-mediated cytotoxicity leading to T cell activation and subsequent target cell lysis. Teclistamab can be used in studies of diseases related to multiple myeloma (MM) .
KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOS highcells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8 + TEffcells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response .
Cibisatamab (CEA-TCB), a T cell bispecific antibody, binds Carcino-Embryonic Antigen (CEA) on cancer cells and CD3 on T cells. Cibisatamab (CEA-TCB) triggers T cell killing of cancer cell lines expressing moderate to high levels of CEA at the cell surface. Cibisatamab (CEA-TCB) can be used for colorectal cancer research .
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) .
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on T cells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces T cell activation and proliferation .
Priliximab (CEN 000029) is an anti-CD4 humanized monoclonal antibody. Priliximab binds to CD4 on the surface of T cells, resulting in a significant and sustained reduction in circulating CD4 +T cells. Priliximab can be used in research of rheumatoid arthritis (RA) .
Tebotelimab (MGD-013) is a humanized IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity .
Cevostamab (BFCR4350A; RG6160; RO7187797) is a humanized IgG1-based BsAb that targets membrane-proximal extracellular domain of FcRH5 on multiple myeloma (MM) cells as well as CD3 on T cells. Moreover, Cevostamab facilitates efficient synapse formation, improves killing activity of T cells against MM tumor cells .
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell 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 .
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 T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment .
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
Dargistotug (M-6223) is a fully human IgG1 monoclonal antibody targeting TIGIT (T cell immune receptor with Ig domain and ITIM). TIGIT is an inhibitory immune checkpoint that promotes NK cell depletion and reduces the secretion of cytokines by binding to CD155 and other antibodies. It can also directly or indirectly inhibit effector T cells and upregulate Tregs cells, thereby exerting immunosuppression. Function .
Tepoditamab (MCLA-117) is a bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab (MCLA-117) kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells and can be used in acute myeloid leukaemia (AML) research .
Telazorlimab (GBR-830) is a humanized monoclonal antibody against OX40 costimulatory receptor on activated T cells. Telazorlimab can be used for the research of autoimmune diseases .
Gotistobart (ONC-392) is a humanized anti-CTLA-4 antibody that confers immunotherapeutic effect by selective depletion of regulatory T cells (Treg) in the tumor microenvironment .
Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .
Vibostolimab is an anti-TIGIT(T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
Renvistobart is an immunoglobulin G1-κ, anti-[Homo sapiens TIGIT (T cell immunoreceptor with Ig domain and ITIM, VSIG9, VSTM3)] Homo sapiens monoclonal antibody .
Muromonab is a monoclonal antibody targeting the CD3 receptor. Muromonab can block all cytotoxic T cell function. Muromonab also as an immunosuppressant agent given to reduce acute solid organ transplant rejection .
Pateclizumab (MLTA3698A) is a humanized antibody against lymphotoxin α (LTα), a transiently expressed cytokine on activated B and T cells (Th1, Th17), which are implicated in rheumatoid arthritis (RA) pathogenesis .
Ipilimumab is a fully human monoclonal antibody IgG1κ that blocks the inhibitory receptor cytotoxic T lymphocyte antigen 4 (CTLA-4) on T cells. Ipilimumab can be used in unresectable or metastatic melanoma (MM) studies .
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease .
Feladilimab (Anti-ICOS/CD278 Reference Antibody (feladilimab); GSK3359609) is humanized IgG4 anti-ICOS agonist monoclonal antibody. Feladilimab binds to ICOS-expressing T cells. Feladilimab has the potential for the research of cancer .
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer .
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 T cell subsets and T regulatory cells .
Theralizumab (TGN1412) is a humanized lgG4 superagonistic anti-CD28 monoclonal antibody that directly stimulates T cells. Theralizumab can cause cytokine release syndrome (CRS). Theralizumab can be used for the research of rheumatoid arthritis .
Ivuxolimab is an OX40 (also known as CD134; TNFRSF4) agonist monoclonal antibody. OX40 is a costimulatory receptor expressed on activated CD4 + and CD8 +T cells. Ivuxolimab shows antitumor activity, with potential immunostimulatory activity .
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activated T cells, NK cells, B cells and plasmacytoid dendritic cells .
Vibecotamab (XmAb14045) is a potent bispecific antibody against CD123 and CD3 that stimulates T cell-mediated targeted killing of CD123-expressing cells. Vibecotamab has antitumor activity and can be used in acute myeloid leukaemia studies .
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 T cells. 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 T cells (Tregs) in vitro. Tregalizumab can be used in the research of autoimmune diseases (resulting from insufficient Treg activity) and allergies .
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
Keliximab (SB-210396) is a chimeric human/macaque IgG1 anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research .
Semzuvolimab is a murine IgG1κ antibody, targeting to p55, T cell surface antigen T4/Leu-3 (CD4). Murine CD4 antibodies can neutralize HIV infection and have the potential to inhibit HAART stable HIV infection .
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo .
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity .
Puxitatug is an immunoglobulin G1-κ, anti-[Homo sapiens VTCN1 (Vset domain containing T cell activation inhibitor 1, B7 family member H4, B7H4, B7-H4)] Homo sapiens monoclonal antibody .
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 research. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer .
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
Toralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab, a immunosuppressive agent, has the potential for active systemic lupus erythematosus (SLE) research .
Vopratelimab (JTX-2011) is a humanized immunoglobulin G1-kappa agonist monoclonal antibody that pecifically binds to the Inducible CO-Stimulator of T cells (ICOS). Vopratelimab retains species cross-reactivity with affinities of 0.93 nM to hICOS, 0.46 nM to cynomolgus ICOS, 3.7 nM to rat ICOS, and 0.64 nM to mICOS. Vopratelimab has antitumor immune response .
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) .
Eciskafusp alfa is a programmed cell death 1 (PDCD1, best known as PD-1) cis-targeted IL2v immunocytokine. Eciskafusp alfa preferentially targets antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells and differentiates them towards a novel population of better effectors. Eciskafusp alfa can be used for the research of cancer and chronic infections .
Latikafusp (AMG 256) is a bifunctional fusion protein comprising a PD-1-targeting antibody and IL-21 mutein designed to deliver IL-21 pathway stimulation to PD-1+ cells. Latikafusp is designed to prime and extend the activity of cytotoxic and memory T cells and induce anti-tumor immunity. Latikafusp has the potential for solid tumors research .Latikafusp may lead to the development of immunogenicity-mediated responses .
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
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 T cells via IL2 receptor binding. Lorukafusp alfa has anti-tumor activity .
Heraclenin, a natural furanocoumarin, significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT) .
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-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
Benzosceptrin C is an inhibitor for PD-L1, which promotes programmed cell death ligand (PD-L1) degradation in a lysosomal pathway, enhances the cytotoxicity of T-cells and exhibits antitumor activity .
Sydowimide A is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), T-cell protein tyrosine phosphatase (TCPTP) and leukocyte common antigen (CD45), with IC50 values of 1.5, 2.4 and 18.83 μM, respectively .
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
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-κB activation 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 .
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 T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype .
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
Tulipalin A (α-Methylene butyrolactone) is a glycoside. Tulipalin A is a causative allergen that induces Allergic contact dermatitides . Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells .
Prostaglandin B2 is a prostaglandin. Prostaglandin B2 is the main substance in cord blood mesenchymal stem cells, to inhibit DC-T Cell proliferation. Prostaglandin B2 also induces cutaneous vasoconstriction of the canine hind paw .
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases .
Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil . Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat .
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent .
9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively .
Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
PD-1/ PD-L1-in-38 is a PD-1/PD-L1 inhibitor, which can inhibit the proliferation of tumor cells, promote the secretion of INF-γ by CD8 +T cells, and inhibit the ability of PD-1/PD-L1 signal transduction. PD-1/PD-L1-IN-38 has antitumor activity .
Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4 +T cells and CD11b + macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA . Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM .
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 T cell activation and can be used in cancer immunity research .
(2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8 +T cells and inhibits the signal transduction of PD-1/PD-L1 .
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 T cells 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 T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
The MLANA protein is essential in melanosome biosynthesis, ensuring the stability of GPR143, and plays a key role in the expression, stability, transport, and processing of the melanocyte protein PMEL. Its interaction with PMEL and GPR143 highlights its integral role in the complex network required for second-stage melanosome formation. MLANA Protein, Human (His, B2M) is the recombinant human-derived MLANA protein, expressed by E. coli , with N-His, B2M labeled tag. The total length of MLANA Protein, Human (His, B2M) is 118 a.a., with molecular weight of ~27.2 kDa.
Linker for Activation of T-cells Family Member 2; Linker for Activation of B-cells; Membrane-Associated Adapter Molecule; Non-T-Cell Activation 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.
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation[1][2].
L-Kynurenine- 13C10 (sulfate hemihydrate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate hemihydrate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype .
HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity .
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 T cell polarization to the anti-inflammatory Treg phenotype .
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat[1]. Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2[2][3][4][5].
Pristane-d40 is the deuterium labeled Pristane[1]. Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil[2]. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat[3].
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 T cell 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].
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
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