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Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab .
Rulonilimab is a human IgG1 monoclonal antibody against PD-1 that targets, binds and inhibits PD-1 and its downstream signalling pathways with potential immune checkpoint inhibition and anti-tumour activity .
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-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
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 .
BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
LAG-3 biner 1 (compound 3) is a small molecule ligand (Kd=1.23 μM) for the immune checkpoint lymphocyte activation gene 3 (LAG-3). LAG-3 biner 1 can be used in the research of cancer diagnosis targeting LAG-3 .
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) .
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 .
Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blockingcheckpoint inhibitor with antitumor activity .
QM31 (SVT016426), a cytoprotective agent, is a selective inhibitor of Apaf-1. QM31 inhibits the formation of the apoptosome (IC50=7.9μM), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9. QM31 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint .
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y) .
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM .
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpointPD-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 .
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation .
FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .
Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) .
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 .
SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
Firastotug is an IgG1κ antibody targeting CTLA4. CTLA4 is a cytotoxic T lymphocyte-associated protein and a key immune checkpoint in the fields of autoimmunity and cancer .
NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer .
HPK1-IN-39 (Compound 10n) is a selective HPK1 Inhibitor (IC50: 29 nM). HPK1-IN-39 inhibits the phosphorylation of SLP76. HPK1-IN-39 can be used for research of cancer immunotherapy .
M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody targeting CTLA-4 (CTLA-4). Zalifrelimab antagonizes the inhibitory checkpoints of immune cell activation regulated by CTLA-4 signaling .
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis .
CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity .
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity .
NTPO (Nitrilotris methylenephosphonic acid) is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor 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 .
Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response .
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .
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 .
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer .
RIP1 kinase inhibitor 5 (example 1) is a potent inhibitor of RIP1, which is used as a checkpoint kinase to control tumor immunity . RIP1 kinase inhibitor 5 is similar with SIR1-365 (compound 13), which inhibits necrosis and iron death activity .
ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3) .
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 .
IDO1-IN-7 is a highly potent and selective indoleamine-2,3-dioxygenase-1 (IDO1) inhibitor, with an IC50 of 6.1 nM in in the cellular assay (SKOV3). IDO1-IN-7 has immunomodulatory effects. IDO1-IN-7 can be used for the research of cancer .
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader .
HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 µΜ<IC50<0.5 µΜ) and Flt3 (IC50<0.05 µΜ) kinase activities .
Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpoint kinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs) .
Antitumor agent-180 (Compound 13a) is an inhibitor for BUB1 mitotic checkpoint serine/threonine kinase B (BUB1B). Antitumor agent-180 inhibits the proliferation of ccRCC cell Caki-1 with IC50 of 2.047 µM. Antitumor agent-180 induces necrosis and apoptosis in Caki-1 .
PF-3837 is an Mps1 kinase inhibitor with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. PF-3837 interferes with the cell cycle checkpoint by inhibiting Mps1 catalytic activity, reducing genomic stability, thereby inducing cancer cell apoptosis (Apoptosis). PF-3837 can be used in research on breast cancer .
ZINC05626394 is a cytochrome b5 reductase 3 inhibitor with activity by increasing nitric oxide bioavailability. ZINC05626394 may have potential applications in anti-cancer suppression, especially in combination with antibody drug conjugates (ADCs) and immune checkpoint inhibitors. The efficacy of ZINC05626394 may be limited by different mechanisms, including antigen-related resistance and failure of endocytosis .
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies .
proTAME, a cell-permeable proagent form of TAME, is an anaphase promoting complex/cyclosome (APC/C) inhibitor. proTAME causes cell cycle arrest in metaphase .
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect .
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity .
Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpoint kinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM) .
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
OM137 is an aurora kinase inhibitor, with an IC50 of 21.7 μM (Aurora A kinase) and 2.4 μM (Aurora B kinase). OM137 also inhibits Cdk1/cyclinB and Cdk5/p25 with an approximate IC50 of 20 μM. OM137 reduces spindle checkpoint-signaling proteins (Mad2 and BubR1) at the kinetochores of chromosomes .
Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases .
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
GW814408X is a kinase chemical genome group (KCGS) compound that inhibits the AURKC kinase involved in cell cycle progression, checkpoint regulation, and cell division. GW814408X exhibits cell line-dependent toxicity, e.g., cytotoxic effects on HeLa cells. GW814408X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
Quinacrine (Acriquine) acetate is a small molecule modulator of the cGAS-STING-TBK1 signaling pathway, possessing immune stimulatory activity. Quinacrine acetate has been explored for its potential therapeutic applications in enhancing anti-tumor immunity. Quinacrine acetate can improve the effectiveness of cancer immunotherapies by addressing the poor immunogenicity of various tumors. Quinacrine acetate also presents a promising strategy for overcoming the limitations associated with immune checkpoint inhibitors in cancer treatment.
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 .
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity .
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity .
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
BMS-242 is a small molecule PD-1/PD-L1 inhibitor with the activity of inhibiting the PD-1/PD-L1 interaction. BMS-242 can bind to the hydrophobic channel pocket between PD-L1 molecules, inhibit the PD-1/PD-L1 immune checkpoint pathway, and provide a new way for cancer inhibition.
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 .
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .
Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
PF-7006 is an Mps1 kinase inhibitor with a Ki value of 0.27 nM and an IC50 value of 2.5 nM. PF-7006 interferes with cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reducing histone H3 levels, and shortening the duration of mitosis, leading to apoptosis in cancer cells. Combined use of PF-7006 with Palbociclib (HY-50767) increases cancer cell tolerance to PF-7006. PF-7006 can be used for breast cancer research .
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .
7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 .
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .
BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM .
TPPC, a porphyrin cholesterol conjugate, can render cancer cells more sensitive to ICIs. TPPC can enhance photodynamic immunotherapy toward lung cancer .
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 .
AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
Talviraline is a non-nucleoside reverse transcriptase (NNRT) inhibitor that is primarily used to inhibit the replication of human immunodeficiency virus type 1 (HIV-1). Talviraline inhibits the viral replication process by binding to a specific site of HIV-1 reverse transcriptase (RT). Talviraline can be used to study the potential countermeasures and safety of HIV-1 infection .
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 2,114 cell cycle/DNA damage-related compounds which can be used in the research of the same.
Immuno-Oncology is a type of immunotherapy that has the specific purpose of treating cancer. It works by stimulating our immune system to fight back. Normally, our immune system is able to destroy cancer cells in our body, however sometimes cancer cells can adapt and mutate, effectively hiding from our immune system. This is when tumors can develop and become a threat to our health. Immuno-oncology involves mobilizing lymphocytes to recognize and eliminate cancer cells using the body’s immune system. There are several immuno-oncology treatments available, including Immune cell therapy (CAR-T), monoclonal antibodies (mABs) and checkpoint inhibitors, cytokines and cancer vaccines.
MCE Small Molecule Immuno-Oncology Compound Library offers 502 bioactive tumor immunology compounds that target some important checkpoints such as PD1/PD-L1, CXCR, Sting, IDO, TLR, etc. This library is a useful tool for Immuno-oncology research.
Gastric Cancer (GC) is one of the most common malignant tumors in the world, ranking fourth in mortality rate globally. Because the early symptoms of stomach neoplasm are usually not obvious, are diagnosed with gastric cancer at terminal stage, and the relative survival rate within 5 years is very low. With the further understanding of the molecular characteristics of stomach neoplasm, many therapeutic targets for gastric cancer have been identified, and molecular targeted therapies such as CTLA-4, HER2 and immune checkpoint inhibitors have made rapid progress. Although survival rates for patients with gastric neoplasm have improved over the past few decades, the prognosis is still worrying. Therefore, there is an urgent need for new drugs to treat gastric cancer.
MCE designs a unique collection of 655 small molecules with definite or potential anti-gastric cancer activity, which is an important tool for studying the pathological mechanism of stomach neoplasm and developing drugs for stomach neoplasm.
NTPO trisodium is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO trisodium are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpoint kinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs) .
Ziptide is a substrate for MAPK activated protein kinase 2 (MAPKAPK2, Km = 5 μM), MAPKAPK3 (Km = 30 μM), PARK (Km = 40 μM), checkpoint kinase 1 (Chk1, Km = 5 μM), AMP-activated protein kinase (AMPK, Km = 75 μM), and calcium/calmodulin-dependent protein kinase II (CamKII, Km = 300 μM) .
Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab .
Rulonilimab is a human IgG1 monoclonal antibody against PD-1 that targets, binds and inhibits PD-1 and its downstream signalling pathways with potential immune checkpoint inhibition and anti-tumour activity .
Lesabelimab (LDP) is an immunoglobulin G1-kappa anti-CD274 monoclonal antibody. CD274 is an immune checkpoint ligand, represses antitumour immunity through the interaction with PDCD1 receptor .
Tinurilimab (Bay 1834942) is an anti-CEACAM6 monoclonal antibody. CEACAM6 is an immune checkpoint regulator suppressing the activity of effector T-cells against tumors .
Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blockingcheckpoint inhibitor with antitumor activity .
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) .
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor .
Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) .
Firastotug is an IgG1κ antibody targeting CTLA4. CTLA4 is a cytotoxic T lymphocyte-associated protein and a key immune checkpoint in the fields of autoimmunity and cancer .
Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody targeting CTLA-4 (CTLA-4). Zalifrelimab antagonizes the inhibitory checkpoints of immune cell activation regulated by CTLA-4 signaling .
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 .
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 .
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 .
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 .
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
The CHEK2 protein is a serine/threonine protein kinase that critically coordinates checkpoint-mediated cell cycle arrest, DNA repair activation, and apoptosis in response to DNA double-strand breaks. Activated CHEK2 phosphorylates CDC25A, CDC25B, and CDC25C, inhibiting their phosphatase activities and preventing the CDK-cyclin complex from activating cell cycle progression. CHEK2 Protein, Human (sf9, GST) is the recombinant human-derived CHEK2 protein, expressed by Sf9 insect cells , with GST labeled tag.
MAD2L1 is a critical spindle assembly checkpoint component that delays anaphase until correct chromosome alignment. During prophase, it forms a heterotetrameric complex with MAD1L1 at unattached kinetochores, recruiting O-MAD2 and aiding transformation. MAD2L1 Protein, Human (His-SUMO) is the recombinant human-derived MAD2L1 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.
CHEK2 is a serine/threonine protein kinase that coordinates cellular responses to DNA double-strand breaks by activating cell cycle arrest, DNA repair, and apoptosis. It phosphorylates effectors and inhibits CDC25A, CDC25B, and CDC25C, thereby enhancing CDK cyclin inhibition and cell cycle arrest. CHEK2 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived CHEK2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of CHEK2 Protein, Mouse (sf9, His-GST) is 546 a.a., with molecular weight of ~90 kDa.
CHFR; E3 ubiquitin-protein ligase CHFR; Checkpoint with forkhead and RING finger domains protein; RING finger protein 196; RING-type E3 ubiquitin transferase CHFR
The CHFR protein is an E3 ubiquitin protein ligase that delays mitosis by microtubule toxicants. CHFR Protein, Human is the recombinant human-derived CHFR protein, expressed by E. coli , with tag free. The total length of CHFR Protein, Human is 663 a.a., .
CHFR; E3 ubiquitin-protein ligase CHFR; Checkpoint with forkhead and RING finger domains protein; RING finger protein 196; RING-type E3 ubiquitin transferase CHFR
The CHFR protein is an E3 ubiquitin protein ligase that delays mitosis by microtubule toxicants. CHFR Protein, Human (His) is the recombinant human-derived CHFR protein, expressed by E. coli , with N-6*His labeled tag. The total length of CHFR Protein, Human (His) is 663 a.a., .
The TRIP13 protein plays a key role in meiosis, affecting chromosome reorganization and structural development. It is critical for the formation of crossing and noncrossing pathways, homologous synapses, and synaptonemal complexes. TRIP13 Protein, Human (His, Strep) is the recombinant human-derived TRIP13 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of TRIP13 Protein, Human (His, Strep) is 432 a.a., .
The TRIP13 protein plays a key role in meiosis, affecting chromosome reorganization and structural development. It is critical for the formation of crossing and noncrossing pathways, homologous synapses, and synaptonemal complexes. TRIP13 Protein, Human is the recombinant human-derived TRIP13 protein, expressed by E. coli , with tag free. The total length of TRIP13 Protein, Human is 432 a.a., .
Chk1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 54 kDa, targeting to Chk1. It can be used for WB,ICC/IF,IP assays with tag free, in the background of Human, Mouse, Rat.
Phospho-Chk2 (Thr68) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 61 kDa, targeting to Phospho-Chk2 (Thr68). It can be used for WB,ICC/IF,IHC-P assays with tag free, in the background of Human, Mouse, Rat.
BUB3 Antibody (YA2180) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2180), targeting BUB3, with a predicted molecular weight of 37 kDa (observed band size: 40 kDa). BUB3 Antibody (YA2180) can be used for WB, IHC-P, ICC/IF, IP, FC experiment in human, mouse, rat background.
BUB1B; BUBR1; MAD3L; SSK1; Mitotic Checkpoint serine/threonine-protein kinase BUB1 beta; MAD3/BUB1-related protein kinase; hBUBR1; Mitotic Checkpoint kinase MAD3L; Protein SSK1
WB, ICC/IF, IP
Human
BUBR1 Antibody (YA2757) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2757), targeting BUBR1, with a predicted molecular weight of 120 kDa (observed band size: 120 kDa). BUBR1 Antibody (YA2757) can be used for WB, ICC/IF, IP experiment in human background.
Phospho-Rad17 (Ser656) Antibody (YA2640) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2640), targeting Phospho-Rad17 (Ser656), with a predicted molecular weight of 77 kDa (observed band size: 80 kDa). Phospho-Rad17 (Ser656) Antibody (YA2640) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human background.
MAD2L1; MAD2; Mitotic spindle assembly Checkpoint protein MAD2A; HsMAD2; Mitotic arrest deficient 2-like protein 1; MAD2-like protein 1
WB
Human
MAD2L1 Antibody (YA1692) is a biotin-conjugated non-conjugated IgG antibody, targeting MAD2L1, with a predicted molecular weight of 24 kDa (observed band size: 24 kDa). MAD2L1 Antibody (YA1692) can be used for WB experiment in human background.
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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