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Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates Tcellproliferation and activation .
CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of Tcells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .
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 Tcellproliferation and in vivo models of arthritis .
Heraclenin, a natural furanocoumarin, significantly inhibits Tcell receptor-mediated proliferation in human primary Tcells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT) .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes Tcells, decreases Tcell activation, inhibites Tcellproliferation and enriches naïve and bona fide regulatory Tcells .
Cortodoxone (Standard) is the analytical standard of Cortodoxone. This product is intended for research and analytical applications. Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates Tcellproliferation and activation .
PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (KD: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC50: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8 +Tcells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cellproliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates Tcell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1 .
HVEM(14-39) is a B- and T-lymphocyte attenuator (BTLA) peptide inhibitor. HVEM (14-39) can be combined with BTLA with a KD of 0.102 μM. HVEM(14-39) enhances the activation and proliferation of Tcells by regulating the expression of BTLA and HVEM in Tcells, and promotes the transformation of cells into effector memory Tcells. HVEM(14-39) inhibits tumor cellproliferation and promotes late apoptosis. HVEM(14-39) has immunomodulatory effects and can be used in the study of cancer .
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 Tcells (NFAT) and T-cellproliferation with an IC50 of ~5 μM. Anti-inflammatory activity .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on Tcells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces Tcell activation and proliferation .
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases Tcell and B cellproliferation.
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 .
VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cellT-47D, induces apoptosis in T-47D .
Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on Tcells. Glofitamab leads to T-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 non-Hodgkin lymphoma (B-NHL) .
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-cellproliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
CSK-IN-1 (compound 13) 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. CSK-IN-1 shows the ability to increase Tcellproliferation induced by Tcell receptor signaling .
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cellproliferation 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 .
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 Tcellproliferation .
FQI1 is a Late SV40 Factor (LSF) inhibitor. FQI1 inhibits cellproliferation, with IC50s of 3, 0.79, 6.3 μM for NIH/3T3, HeLa, A549 cells. FQI1 can be used for cancer research .
Teriflunomide (Standard) is the analytical standard of Teriflunomide. This product is intended for research and analytical applications. Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases Tcell and B cellproliferation.
EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cellproliferation and has antitumor activity .
UG-650 is a non-Gemini analog of UVB1 that combines the structural features of UVB1 and MC 1288. UG-650 can bind to the vitamin D receptor (VDR) and inhibit the proliferation of MCF-7 cells and the migration of MC3T3-E1 cells .
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent Tcellproliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human Tcells, respectively .
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ Tcellproliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
Prostaglandin B2 is a prostaglandin. Prostaglandin B2 is the main substance in cord blood mesenchymal stem cells, to inhibit DC-TCellproliferation. Prostaglandin B2 also induces cutaneous vasoconstriction of the canine hind paw .
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-cellproliferation 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-cellproliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
PTP1B-IN-30 (Compound 3j) is the inhibitor for PTP1B with an IC50 of 0.51 µM. PTP1B-IN-30 inhibits the proliferation of cancer cellT47D with an IC50 of 21.21 µM, arrests the cell cycle at S phase, and induces apoptosis in T47D .
EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
Remisporine B is a polyketide, that can be isolated from Penicillium sp. ZJ-SY2. Remisporine B exhibits immunosuppressive efficacy, that inhibits concanavalin A (HY-P2149)-induced T-cellproliferation and LPS (HY-D1056)- induced B-cellproliferations of mouse splenic lymphocytes with IC50 of 30.1 µg/mL and 32.4 µg/mL .
Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating Tcell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA .
Steroid sulfatase-IN-5 (compound 10b) is a steroid sulfatase (STS) inhibitor (IC50: 0.32 nM). Steroid sulfatase-IN-5 inhibits T-47D cellproliferation with an IC50 of 35.7 μM. Steroid sulfatase-IN-5 can be used for research of breast cancer .
Vabametkib is a potent inhibitor of hepatocyte growth factor receptor (HGFR). Vabametkib inhibits Hs746Tcellsproliferation and inhibits c-Met with an IC50 value of 7 nM. Vabametkib can be used as an antineoplastic agent .
KV1.3-IN-1 (Compound trans-18) is a KV1.3 channel inhibitor (IC50: 230 nM and 26.12 nM in Ltkcells 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 .
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 cellproliferation and mediates apoptosis. Caerin 1.1 TFA may enhance adaptive Tcell immune responses .
Myelin Basic Protein(87-99) TFA is an encephalitogenic peptide that induces basic protein-specific Tcellproliferation. Myelin Basic Protein(87-99) TFA causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS) .
Atiprimod (Azaspirane) (dimaleate) is an anti-proliferative and anti-angiogenic agent that inhibits proliferation of cancer cell lines. Atiprimod (dimaleate) also induces Apoptosis and activates both caspase-9 and caspase-3 in T84 colon carcinoma cells. Atiprimod (dimaleate) inhibits both bFGF and VEGF induced proliferation and migration of human umbilical vein endothelial cells, resulting in disruption of cord formation. Atiprimod (dimaleate) reduces production of IL-6, VEGF and inhibits activation of Stat3 .
LF 1695 is an immunomodulator. LF 1695 enhances the proliferative response of T cells by increasing the production of IL2 (interleukin-2) or the expression of the IL2 receptor. LF 1695 also increases CONA-induced inhibitory activity in human lymphocytes. LF 1695 can be used to study the proliferative and inhibitory activity of T cell subpopulations, as well as their role in immune regulation .
Immunosuppressant-1 (Compound 31) inhibits anti-CD3/anti-CD28 co-stimulated T-cellproliferation. Immunosuppressant-1 has immunosuppressive activity, and induces apoptosis by activating caspase-3 and PARP in activated lymph node 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 Tcell differentiation, and inhibits CD4+ Tcellproliferation. 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 .
XMD15-44 is a RET kinase inhibitor.XMD15-44 has a growth-inhibitory effect on RET/C634R and RET/M918T transformed RAT1 cells, with IC50 values of 11.5 nM and 8.3 nM, respectively. XMD15-44 can inhibit RET kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles, reducing cellproliferation .
MG-T-19 is an effective TIM-3 inhibitor that can suppress the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9. MG-T-19 can increase the production of tumor necrosis factor-α (TNF-α) and interferon-γ (IFN-γ) in peripheral blood mononuclear cells (PBMCs) from healthy donors, and enhance the ability of PBMCs to inhibit the proliferation of Kasumi-1 cells (an acute myelogenous leukemia cell line) .
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a Tcellproliferation 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 .
Tubulin polymerization-IN-75 (Compound 6) is an inhibitor for tubulin polymerization with an IC50 of 30 μM. Tubulin polymerization-IN-75 inhibits the proliferation of cancer cell Huh7 and 293T with IC50 of 14.3 μM and 13.8 μM .
NCATS-SM4420 (Compound A35) is an orally active thyroid-stimulating hormone receptor (TSHR) ligand that inhibits the proliferation of MDA-T32 and MDA-T85 cells in vitro (IC50 values of 0.71 μM and 0.38 μM, respectively) and suppresses metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds promise for research in the field of thyroid cancer .
Wnt/β-catenin activator 1 (Compound 5m) is the orally active activator for Wnt/β-catenin signaling pathway, that arrests cell cycle at G1 phase, inhibits early proliferation of adipocytes, and inhibits adipogenesis in cell3T3-L1 with an IC50 of 330 nM. Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities in high-fat diet fed Syrian golden hamster model .
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 Tcellproliferation. GABAA receptor agent 4 has the immunomodulatory potential .
CVRARTR is an antagonist for programmed cell death ligand-1 (PD-L1) with KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and Tcellproliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model .
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 Tcells in vitro .
GR-28 is an inhibitor for small C-terminal domain phosphatase 1 (SCP1). GR-28 inhibits the transcriptional activity of repressor element-1 silencing transcription factor (REST), inhibits the proliferation of glioblastoma cells (IC50 is 2.9 and 10.1 µM, for cells A172 and T98G) .
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
Sp-8-Br-cAMPS sodium is a cAMP analog, which performs a protein kinase A (PKA) activating activity with EC50 of 360 nM. Sp-8-Br-cAMPS sodium inhibits proliferation of Tcells and the haemocyte non-self response in Lepidoptera larve .
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-Tcells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-Tcells .
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 +Tcells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
Terminaline is a compound that can be isolated from Sarcococca saligna. Terminaline has immunosuppressive activity and can inhibit the proliferation of Tcells and the production of IL-2. In vivo, Terminaline can reduce CCl4-induced liver injury and has a good hepatoprotective effect .
EMB-02 is a bispecific PD-1 and LAG-3 antibody. EMB-02 inhibits the PD-1- and LAG-3-mediated downregulation of T-cell activation and proliferation. EMB-02 has a potent anticancer effects .
Aphidicolins B32 is a diterpenoid compound discovered in the marine fungus Botryotinia fuckeliana, exhibiting cytotoxic activity against human bladder cancer cells. It inhibits the proliferation of T24 cells in the G0/G1 phase, with an IC50 of 27.6 μM. Aphidicolins B32 holds potential for research in the field of cancer therapy .
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.
D228 is an orally active antiinflammatory agent. D228 reduces ConA induced T lymphocyte cellproliferation (IC50: 42.85 μM) and LPS induced B lymphocyte cellproliferation (IC50: 3.15 μM). D228 is effective against inflammatory bowel disease (IBD). D228 alleviates the DSS (HY-116282C)-induced inflammation response in the IBD model by downregulating the MyD88/TRAF6/p38 signaling .
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 cellproliferation assay .
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM) .
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 Tcellproliferation and inhibits IL-2 production. Keliximab can be used for cancer research .
CD73-IN-19 (Compound 4ab) is a CD73 inhibitor (with a 44% inhibition rate of CD73 enzymatic activity at 100 μM). CD73-IN-19 (at 10 μM and 100 μM) can completely antagonize the blockade of Tcellproliferation induced by TCR (Tcell receptor) triggering (which is induced by CD73 activity), and it can also inhibit the hA2A receptor activity in HEK-293 cells (Ki is 3.31 μM). CD73-IN-19 holds promise for research in the field of immune diseases .
Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation .
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cellproliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research .
M351-0056 is the agonist for the immune checkpoint protein VISTA, that reduces the secretion of VISTA-induced cytokines, promotes the T-cellproliferation induced by VISTA, and exhibits immunomodulatory activity. M351-0056 ameliorates Imiquimod (HY-B0180)-induced psoriatic dermatitis in mouse models .
AT9283 hydrochloride is a multi-targeted kinase inhibitor with anti-tumor activity. AT9283 hydrochloride has been found to effectively inhibit Aurora A and Aurora B kinases, thereby affecting cellproliferation and survival. AT9283 hydrochloride can also inhibit several other kinases, including JAK2 and Abl (T315I) .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797Scells with IC50s of 1.526, 66.7 nM, respectively .
KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response .
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
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 Tcellproliferation. SIRT6-IN-2 has immunosuppressive and chemosensitizing effects .
CD19 CAR circRNA will express CD19 car protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
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 Tcells 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 .
Transketolase-IN-4 is a potent transketolase inhibitor (IC50=3.9 μM). Transketolase-IN-4 inhibits tumor cellproliferation of SW620, LS174T, and MIA PaCa-2. Transketolase-IN-4 is a possible Mycobacterium tuberculosis DXS inhibitor, with an IC50 value of 114.1 μM .
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
GPX4-IN-13 (compound 16) is a GPX4 inhibitor with anticancer activity. GPX4-IN-13 reduces thyroid cellproliferation and induces ferroptosis by inhibiting the expression level of GPX4. GPX4-IN-13 inhibits the growth of three thyroid cancer cell lines: N-thy-ori-3-1 (IC50=8.39 μM), MDA-T32 (IC50=10.28 μM) and MDA-T41 (IC50=8.18 μM) .
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-Tcells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-Tcells .
Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cellproliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cellproliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote Tcell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
CD19 CAR mRNA (Mouse) will express mouse CD19 CAR protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 CAR is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
AKT-IN-25 (Compound 14a) is an inhibitor for Akt, that inhibits the phosphorylation of Akt, and thereby inhibits the PI3K/Akt/mTOR signaling pathway. AKT-IN-25 arrests the cell cycle at G1 phase, inhibits the cell migration of PANC-1, and inhibits the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2 with IC50s of 3.05, 1.32, and 3.85 μM, respectively .
CD19 CAR mRNA (Human) will express Human CD19 CAR protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 CAR is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cellproliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
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 Tcells. DGKα-IN-3 has the potential for cancer and immunology study.
Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC50s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC50 is 74.44 μM), which exhibits anticancer potency .
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 Tcells. 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 Tcells. DGKα-IN-2 has the potential for cancer and immunology study.
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
α-Glucosidase-IN-76 (Compound 4r) is an inhibitor for α-glucosidase with an IC50 of 5.44 μM. α-Glucosidase-IN-76 scavenges ABTS+ free radicals with a TEAC value of 0.49. α-Glucosidase-IN-76 inhibits the proliferation of T24 bladder cancer cell with IC50 of 1.74 μM .
Sp-8-Br-cAMPS is an analog of cAMP(HY-B1511). Sp-8-Br-cAMPS is an agonist for cAMP, which performs a protein kinase A (PKA) activating activity with EC50 of 360 nM. Sp-8-Br-cAMPS inhibits proliferation of Tcells and the haemocyte non-self response in Lepidoptera larve .
Hyaluronan-binding peptide, biotin labeled TFA 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 Tcellproliferation.) .
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 +Tcells, and inhibit the ability of PD-1/PD-L1 signal transduction. PD-1/PD-L1-IN-38 has antitumor activity .
CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cellproliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a xenograft model .
[Ru(phen)2(HMPIP)](PF6)2 (Compound 6A) is an anti-tumor agent. [Ru(phen)2(HMPIP)](PF6)2 can inhibit the proliferation and migration of HepG2 liver cancer cells, and induce apoptosis, autophagy, cell cycle arrest and ferroptosis of HepG2 liver cancer cells. [Ru(phen)2(HMPIP)](PF6)2 exerts its anti-tumor activity by stimulating immune response to increase CD8+ Tcells .
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
Nogapendekin alfa (his tag), a soluble protein subunit of a human interleukin (IL)-15 variant, is a superagonist of IL-15. Nogapendekin alfa (his tag) promotes the proliferation and viability of immune cells. Nogapendekin alfa (his tag) combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form N-803 (Nogapendekin alfa inbakicept), an IL-15 cytokine antibody fusion protein. N-803 reduces tumor burden by activation of NK cells and CD8 +Tcells .
1,1′-Ethylidenebis[L-tryptophan] is an impurity in the synthesis of L-tryptophan. 1,1′-Ethylidenebis[L-tryptophan] promotes the proliferation of eosinophilic leukemia cells, induces the release of eosinophil cationic protein from eosinophils, and stimulates Tcells to produce IL-5. 1,1′-Ethylidenebis[L-tryptophan] (40 µg/kg) can induce fascia thickening, mast cell infiltration, and fibrosis in adipose and subcutaneous muscle tissues in mice. 1,1′-Ethylidenebis[L-tryptophan] can be used in immunology and inflammation research .
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
BTN3A1 ligand-1 (Compound 26b) is a triazole-containing aryl/acyloxyalkyl phosphonate prodrug. BTN3A1 ligand-1 can stimulate Tcellproliferation (EC50: 0.49 nM) and interferon γ secretion. BTN3A1 ligand-1 has certain plasma stability and can be used in related immunotherapy research .
Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cellapoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2 .
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-cellproliferation in vivo and has the potential for autoimmune disease research .
BMS-243117 is a potent, and selective benzothiazole based p56 Lck inhibitor with an IC50 of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC50 of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck .
EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cellapoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
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 cellproliferation 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 .
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
VGB3 is an antagonist peptide of vascular endothelial growth factor receptor 1 (VEGFR1)/VEGFR2 with antiangiogenic and antitumor effects. VGB3 binds to both VEGFR1 and VEGFR2, thereby inhibits VEGF-driven proliferation, migration and tube formation of endothelial cells, and tumor growth and metastasis in murine 4T1 mammary carcinoma tumor 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-cellproliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
WRR-483 is an analog of K11777, an inhibitor of cruzain, used to inhibit the proliferation of Trypanosoma cruzi in cell culture. WRR-483 can eradicate parasitic infection in an acute Chagas disease mouse model. WRR-483 is an irreversible cysteine protease inhibitor that shows pH-dependent high affinity and potent trypanocidal activity against cruzain and T. cruzi infection, and is expected to inhibit Chagas disease.
DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cellproliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote Tcell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
CD19 car mRNA (Mouse)-LNP is a lipid nanoparticle (LNP) containing CD19 car mRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car mRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
CD19 car circRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car circRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car circRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cellproliferation and transformation in breast cancer cells .
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cellproliferation and induction of apoptosis .
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
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-cellproliferation 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 .
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cellproliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
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 Tcellproliferation, is a promising tool for study autoimmune diseases .
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293Tcells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cellproliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cellsproliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .
Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cellapoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2 .
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+ Tcells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cellsproliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cellproliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cellproliferation and has anticancer activity .
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-cellproliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development .
HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET .
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat Tcells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants .
Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cellproliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cellproliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WTIC50=281 nM, c-MET IC50=205 nM, B-RAF WTIC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790MIC50=69 nM and B-RAF V600EIC50=83 nM) .
Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cellproliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cellsproliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . 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 Tcell activation and increases IL-2 production in primary human TCells . NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
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-cellproliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity .
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of Tcells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293Tcells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
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 293Tcells (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 .
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances Tcell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy .
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation.
CD19 car mRNA (Mouse)-LNP is a lipid nanoparticle (LNP) containing CD19 car mRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car mRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
CD19 car circRNA-LNP is a lipid nanoparticle (LNP) containing CD19 car circRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car circRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
Myelin Basic Protein(87-99) TFA is an encephalitogenic peptide that induces basic protein-specific Tcellproliferation. Myelin Basic Protein(87-99) TFA causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS) .
CVRARTR is an antagonist for programmed cell death ligand-1 (PD-L1) with KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and Tcellproliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model .
Hyaluronan-binding peptide, biotin labeled TFA 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 Tcellproliferation.) .
HVEM(14-39) is a B- and T-lymphocyte attenuator (BTLA) peptide inhibitor. HVEM (14-39) can be combined with BTLA with a KD of 0.102 μM. HVEM(14-39) enhances the activation and proliferation of Tcells by regulating the expression of BTLA and HVEM in Tcells, and promotes the transformation of cells into effector memory Tcells. HVEM(14-39) inhibits tumor cellproliferation and promotes late apoptosis. HVEM(14-39) has immunomodulatory effects and can be used in the study of cancer .
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 .
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific Tcellproliferation. Myelin Basic Protein(87-99) 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 cellproliferation and mediates apoptosis. Caerin 1.1 TFA may enhance adaptive Tcell immune responses .
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a Tcellproliferation 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 .
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 Tcellproliferation.)
IT9302 is a synthetic IL-10 agonist with the activity of inducing tolerogenic dendritic cells. IT9302 is able to mimic multiple effects of IL-10, including downregulating the antigen presentation machinery and increasing the sensitivity of tumor cells to natural killer cell-mediated lysis. IT9302 can also hinder the response of human monocytes to differentiation factors and reduce the antigen presentation and co-stimulatory capacity of dendritic cells. Dendritic cells treated with IT9302 showed a weakened ability to stimulate Tcellproliferation and interferon-γ production. IT9302 exerts its effects through mechanisms that are partially different from IL-10, involving STAT3 inactivation and regulation of the NF-κB intracellular pathway. IT9302-treated dendritic cells showed enhanced expression of membrane-bound TGF-β, associated with the effective induction of foxp3+ regulatory Tcells .
VGB3 is an antagonist peptide of vascular endothelial growth factor receptor 1 (VEGFR1)/VEGFR2 with antiangiogenic and antitumor effects. VGB3 binds to both VEGFR1 and VEGFR2, thereby inhibits VEGF-driven proliferation, migration and tube formation of endothelial cells, and tumor growth and metastasis in murine 4T1 mammary carcinoma tumor model .
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+ Tcells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes Tcells, decreases Tcell activation, inhibites Tcellproliferation and enriches naïve and bona fide regulatory Tcells .
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on Tcells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces Tcell activation and proliferation .
Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on Tcells. Glofitamab leads to T-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 non-Hodgkin lymphoma (B-NHL) .
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 Tcellproliferation and inhibits IL-2 production. Keliximab can be used for cancer research .
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-cellproliferation 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 .
EMB-02 is a bispecific PD-1 and LAG-3 antibody. EMB-02 inhibits the PD-1- and LAG-3-mediated downregulation of T-cell activation and proliferation. EMB-02 has a potent anticancer effects .
Nogapendekin alfa (his tag), a soluble protein subunit of a human interleukin (IL)-15 variant, is a superagonist of IL-15. Nogapendekin alfa (his tag) promotes the proliferation and viability of immune cells. Nogapendekin alfa (his tag) combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form N-803 (Nogapendekin alfa inbakicept), an IL-15 cytokine antibody fusion protein. N-803 reduces tumor burden by activation of NK cells and CD8 +Tcells .
Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates Tcellproliferation and activation .
Heraclenin, a natural furanocoumarin, significantly inhibits Tcell receptor-mediated proliferation in human primary Tcells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT) .
Prostaglandin B2 is a prostaglandin. Prostaglandin B2 is the main substance in cord blood mesenchymal stem cells, to inhibit DC-TCellproliferation. Prostaglandin B2 also induces cutaneous vasoconstriction of the canine hind paw .
Cortodoxone (Standard) is the analytical standard of Cortodoxone. This product is intended for research and analytical applications. Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates Tcellproliferation and activation .
Remisporine B is a polyketide, that can be isolated from Penicillium sp. ZJ-SY2. Remisporine B exhibits immunosuppressive efficacy, that inhibits concanavalin A (HY-P2149)-induced T-cellproliferation and LPS (HY-D1056)- induced B-cellproliferations of mouse splenic lymphocytes with IC50 of 30.1 µg/mL and 32.4 µg/mL .
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 Tcell differentiation, and inhibits CD4+ Tcellproliferation. 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 .
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
Terminaline is a compound that can be isolated from Sarcococca saligna. Terminaline has immunosuppressive activity and can inhibit the proliferation of Tcells and the production of IL-2. In vivo, Terminaline can reduce CCl4-induced liver injury and has a good hepatoprotective effect .
Aphidicolins B32 is a diterpenoid compound discovered in the marine fungus Botryotinia fuckeliana, exhibiting cytotoxic activity against human bladder cancer cells. It inhibits the proliferation of T24 cells in the G0/G1 phase, with an IC50 of 27.6 μM. Aphidicolins B32 holds potential for research in the field of cancer therapy .
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 cellproliferation assay .
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 +Tcells, and inhibit the ability of PD-1/PD-L1 signal transduction. PD-1/PD-L1-IN-38 has antitumor activity .
Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cellapoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2 .
Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cellapoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2 .
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
UBE2T Protein, an essential ubiquitination component, serves as an E2 ubiquitin-conjugating enzyme, accepting ubiquitin from the E1 complex and catalyzing its covalent attachment to proteins. This multifaceted enzyme catalyzes monoubiquitination, crucial in MMC-induced DNA repair processes. Its significance is highlighted by specific association with the Fanconi anemia complex, collaborating with FANCL for FANCD2 monoubiquitination in the DNA damage response pathway. Beyond DNA repair, UBE2T mediates monoubiquitination of FANCL and FANCI and potentially contributes to BRCA1 ubiquitination and degradation. In vitro, UBE2T promotes various polyubiquitination types, showcasing involvement in diverse ubiquitin-dependent processes. UBE2T Protein, Human (His) is the recombinant human-derived UBE2T protein, expressed by E. coli, with N-6*His labeled tag. The total length of UBE2T Protein, Human (His) is 197 a.a., with molecular weight of 25-30 kDa.
The MTCP1 protein plays a crucial role in promoting the phosphorylation and activation of AKT1 and AKT2, two key members of the AKT family. It does this through specific interactions with AKT1 and AKT2, primarily through their PH (pleckstrin homology) domains. MTCP1 Protein, Human is the recombinant human-derived MTCP1 protein, expressed by E. coli , with tag free. The total length of MTCP1 Protein, Human is 107 a.a., .
The MTCP1 protein plays a crucial role in promoting the phosphorylation and activation of AKT1 and AKT2, two key members of the AKT family. It does this through specific interactions with AKT1 and AKT2, primarily through their PH (pleckstrin homology) domains. MTCP1 Protein, Human (His, Strep) is the recombinant human-derived MTCP1 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of MTCP1 Protein, Human (His, Strep) is 107 a.a., .
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293Tcells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cellsproliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CD19 CAR mRNA (Mouse) will express mouse CD19 CAR protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 CAR is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
CD19 CAR mRNA (Human) will express Human CD19 CAR protein, and can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 CAR is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction.
CD19 car mRNA (Mouse)-LNP is a lipid nanoparticle (LNP) containing CD19 car mRNA, suitable for detection of RNA delivery, translation efficiency, cell viability, etc. CD19 car mRNA can be used in chimeric antigen receptor Tcell immunotherapy (CAR-CD19). The CD19 car is a chimeric antigen receptor. Among them, CD19 is a CD molecule expressed by B cells (i.e. leukocyte differentiation antigen), an important membrane antigen involved in B cellproliferation, differentiation, activation and antibody production, and can also promote BCR signal transduction .
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