Search Result

Results for "

immune microenvironment

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (3) Arginase (1) Bcl-2 Family (1) c-Fms (3) c-Kit (2) CCR (1) CD74 (1) Checkpoint Kinase (Chk) (1) CXCR (1) Discoidin Domain Receptor (2) DNA Methyltransferase (1) Endogenous Metabolite (2) ERK (2) FGFR (1) FLT3 (2) HDAC (2) HSP (1) IFNAR (1) Integrin (1) Interleukin Related (1) MEK (1) METTL3 (1) NO Synthase (1) PD-1/PD-L1 (6) Phosphodiesterase (PDE) (1) PKD (1) Protein Arginine Deiminase (2) Raf (1) Ras (2) Reactive Oxygen Species (2) STAT (2) STING (3) TGF-β Receptor (1) Tie (1) Toll-like Receptor (TLR) (3) Trk Receptor (2) VEGFR (4) VISTA (1)
By Research Areas:	Cancer (29) Infection (1) Inflammation/Immunology (9) Metabolic Disease (2)

By Targets:

Akt (1)

Apoptosis (3)

Arginase (1)

Bcl-2 Family (1)

c-Fms (3)

c-Kit (2)

CCR (1)

CD74 (1)

Checkpoint Kinase (Chk) (1)

CXCR (1)

Discoidin Domain Receptor (2)

DNA Methyltransferase (1)

Endogenous Metabolite (2)

ERK (2)

FGFR (1)

FLT3 (2)

HDAC (2)

HSP (1)

IFNAR (1)

Integrin (1)

Interleukin Related (1)

MEK (1)

METTL3 (1)

NO Synthase (1)

PD-1/PD-L1 (6)

Phosphodiesterase (PDE) (1)

PKD (1)

Protein Arginine Deiminase (2)

Raf (1)

Ras (2)

Reactive Oxygen Species (2)

STAT (2)

STING (3)

TGF-β Receptor (1)

Tie (1)

Toll-like Receptor (TLR) (3)

Trk Receptor (2)

VEGFR (4)

VISTA (1)

By Research Areas:

Cancer (29)

Infection (1)

Inflammation/Immunology (9)

Metabolic Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-131347

PD-1/PD-L1-IN-NP19	PD-1/PD-L1	Inflammation/Immunology Cancer
PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC₅₀ of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects .

HY-159127

HRS-4642	Ras	Cancer
HRS-4642 is a selective KRAS(G12D) inhibitor (Kd=0.083 nM) with anti-cancer activity. HRS-4642 synergizes with Carfilzomib (HY-10455) and exhibits significant in vivo potency to reshape the tumor microenvironment into an immune-activating microenvironment.

HY-156677

STC-15	METTL3	Cancer
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 .

HY-N6985

Baccatin III 1 Publications Verification	Others	Cancer
Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment[1][2].

HY-154869

PD-1/PD-L1-IN-34	PD-1/PD-L1	Inflammation/Immunology Cancer
PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) inhibits PD-1/PD-L1 interaction (IC₅₀=0.029 μM), with a selected binding affinity with PD-L1 (K_D=0.1554 μM). PD-1/PD-L1-IN-34 inhibits tumor growth by activating the immune microenvironment .

HY-N15169

BG-136	IFNAR CD74 NO Synthase Arginase	Cancer
BG-136 is an innate immune stimulant isolated from Durvillaea Antarctica that can simultaneously stimulate the activation of both innate and adaptive immune cells in the tumor microenvironment (TME), exerting a broad-spectrum antitumor effect .

HY-168088

DNMT1/HDAC-IN-1	HDAC DNA Methyltransferase	Cancer
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC₅₀=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .

HY-157157

PAD4-IN-3	Protein Arginine Deiminase	Cancer
PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment .

HY-168887

ZSA-51	STING	Cancer
ZSA-51 is a potent and orally active STING agonist. ZSA-51 shows anticancer activity. ZSA-51 remodeles immune microenvironment both in tumor and lymph node .

HY-151559

Zn-DPA-maytansinoid conjugate 1	Checkpoint Kinase (Chk) STAT CXCR CCR	Cancer
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" .

HY-119367

ODM-203	FGFR VEGFR	Cancer
ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC₅₀ values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment .

HY-172396

PD-L1/VISTA-IN-2	PD-1/PD-L1 VISTA	Cancer
PD-L1/VISTA-IN-2 (Compound S8) is an orally active bifunctional PD-L1/VISTA inhibitor with an IC₅₀ of 1.4 μM for PD-L1 and a K_D of 2.1 μM for VISTA. PD-L1/VISTA-IN-2 can activate the tumor immune microenvironment and exert anti-cancer effects .

HY-107202

Polyinosinic-polycytidylic acid Maximum Cited Publications 28 Publications Verification Poly(I:C)	Toll-like Receptor (TLR) PKD HSP Bcl-2 Family Interleukin Related	Infection Inflammation/Immunology Cancer
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .

HY-135748

Polyinosinic-polycytidylic acid sodium Maximum Cited Publications 28 Publications Verification Poly(I:C) sodium	Toll-like Receptor (TLR) Apoptosis	Inflammation/Immunology Cancer
Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis .

HY-134958

Polyinosinic-polycytidylic acid potassium Poly(I:C) potassium	Toll-like Receptor (TLR) Apoptosis	Inflammation/Immunology Cancer
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis .

HY-162494

PAD4-IN-4	Protein Arginine Deiminase	Cancer
PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC₅₀=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .

HY-171331

AB-3PRGD2	PD-1/PD-L1 Integrin	Cancer
AB-3PRGD2 is a radiotherapeutic agent targeting integrin α_vβ₃. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8 ⁺ T cells .

HY-B0722

Histamine dihydrochloride 5+ Cited Publications	Endogenous Metabolite Reactive Oxygen Species	Metabolic Disease Cancer
Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-151427

TGFβ1-IN-1 1 Publications Verification	TGF-β Receptor	Inflammation/Immunology
TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies .

HY-148029

Dazostinag disodium TAK-676	STING	Cancer
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .

HY-168491

Enpp-1-IN-25	Phosphodiesterase (PDE) STING PD-1/PD-L1	Cancer
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC₅₀ of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .

HY-16961

Sitravatinib 5 Publications Verification MGCD516; MG-516	VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor	Inflammation/Immunology Cancer
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .

HY-144746

PD-1/PD-L1-IN-26	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC₅₀ of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases .

HY-16961A

Sitravatinib malate MGCD516 malate; MG-516 malate	VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor	Inflammation/Immunology Cancer
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .

HY-B0722R

Histamine (dihydrochloride) (Standard)	Endogenous Metabolite Reactive Oxygen Species	Metabolic Disease Cancer
Histamine (dihydrochloride) (Standard) is the analytical standard of Histamine (dihydrochloride). This product is intended for research and analytical applications. Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .

HY-164529

SJ-C1044	Raf Ras MEK ERK VEGFR Tie c-Fms	Cancer
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .

HY-153358

TNG260	HDAC	Cancer
TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .

HY-158050

PXB17	c-Fms	Cancer
PXB17 can inhibit CSF1R (IC₅₀ = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .

HY-168954

CSF1R-IN-26	c-Fms Apoptosis Akt ERK STAT	Inflammation/Immunology Cancer
CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC₅₀ of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .

Cat. No.	Product Name

HY-L204

Lactic Acid Metabolic Compound Library	399 compounds
Lactic acid metabolism is one of the key metabolic pathways within living organisms. It plays a crucial role not only in cellular energy conversion but is also closely related to a variety of physiological and pathological processes. The production and clearance of lactic acid are important indicators of cellular metabolic balance, and its abnormal regulation may lead to conditions such as lactic acidosis, muscle fatigue, and hereditary metabolic diseases. Moreover, lactic acid is closely related to the malignancy of tumors and is considered a biomarker for malignant tumors and poor prognosis. Lactic acid can serve as a metabolic substrate to support the metabolic needs of tumor cells under hypoxic conditions, and it can also cause acidification of the tumor microenvironment, suppress immune cell function to promote immune evasion, and induce drug resistance in tumor cells. Currently, targeting lactic acid-lactylation and its related metabolic pathways has become a new research avenue for cancer treatment. In-depth exploration of the molecular mechanisms of lactic acid metabolism can help in screening lead compounds that regulate the lactic acid metabolism. MCE contains 399 small molecule compounds targeting enzymes involved in lactic acid metabolism. This library is of significant value for researching the role of lactate metabolism in the mechanisms of diseases.

Lactic Acid Metabolic Compound Library

399 compounds

Lactic acid metabolism is one of the key metabolic pathways within living organisms. It plays a crucial role not only in cellular energy conversion but is also closely related to a variety of physiological and pathological processes. The production and clearance of lactic acid are important indicators of cellular metabolic balance, and its abnormal regulation may lead to conditions such as lactic acidosis, muscle fatigue, and hereditary metabolic diseases. Moreover, lactic acid is closely related to the malignancy of tumors and is considered a biomarker for malignant tumors and poor prognosis. Lactic acid can serve as a metabolic substrate to support the metabolic needs of tumor cells under hypoxic conditions, and it can also cause acidification of the tumor microenvironment, suppress immune cell function to promote immune evasion, and induce drug resistance in tumor cells. Currently, targeting lactic acid-lactylation and its related metabolic pathways has become a new research avenue for cancer treatment. In-depth exploration of the molecular mechanisms of lactic acid metabolism can help in screening lead compounds that regulate the lactic acid metabolism.

MCE contains 399 small molecule compounds targeting enzymes involved in lactic acid metabolism. This library is of significant value for researching the role of lactate metabolism in the mechanisms of diseases.

HY-L213

Anti-Cancer Approved Drug Library	283 compounds
The anti-cancer drug library meticulously collects all drugs approved by FDA and other major national drug regulatory authorities for cancer treatment. These drugs cover a variety of cancer types, including but not limited to lung cancer, breast cancer, colorectal cancer, leukemia, and other common cancers. The library includes a wide range of drugs, from classic chemotherapeutic agents to cutting-edge targeted therapies and immunotherapies. It contains various types of drug compounds with different mechanisms of action. There are cytotoxic drugs that directly kill cancer cells, as well as drugs that work by modulating the tumor microenvironment, inhibiting tumor angiogenesis, and activating the immune system. This diversity provides researchers with a broad range of perspectives and options for intervention strategies. This library can be used for basic research on cancer treatment, exploring new targets and new mechanisms of drug action; Conducting drug reuse research to look for potential therapeutic effects of existing drugs on other cancer types or diseases; Or conducting research into combination drugs to optimize cancer treatment. MCE has collected 283 small-molecule compounds with cancer indications, which are good tools for drug repurposing.

Anti-Cancer Approved Drug Library

283 compounds

The anti-cancer drug library meticulously collects all drugs approved by FDA and other major national drug regulatory authorities for cancer treatment. These drugs cover a variety of cancer types, including but not limited to lung cancer, breast cancer, colorectal cancer, leukemia, and other common cancers. The library includes a wide range of drugs, from classic chemotherapeutic agents to cutting-edge targeted therapies and immunotherapies. It contains various types of drug compounds with different mechanisms of action. There are cytotoxic drugs that directly kill cancer cells, as well as drugs that work by modulating the tumor microenvironment, inhibiting tumor angiogenesis, and activating the immune system. This diversity provides researchers with a broad range of perspectives and options for intervention strategies.

This library can be used for basic research on cancer treatment, exploring new targets and new mechanisms of drug action; Conducting drug reuse research to look for potential therapeutic effects of existing drugs on other cancer types or diseases; Or conducting research into combination drugs to optimize cancer treatment.

MCE has collected 283 small-molecule compounds with cancer indications, which are good tools for drug repurposing.

Cat. No.	Product Name	Target	Research Area

HY-P10449

M2 Peptide	Peptides	Cancer
M2 Peptide is a peptide targeting M2-like tumor-associated macrophages (TAMs). M2 Peptide is used to carry drugs or small interfering RNA (siRNA) to promote the repolarization of M2-like macrophages to M1-like macrophages, thereby altering the immunosuppressive state in the tumor microenvironment and enhancing the anti-tumor immune response. M2 Peptide can be used to study the effect of macrophage polarization and how this polarization change affects tumor growth and metastasis .

Cat. No.	Product Name	Category	Target	Chemical Structure