The immune system has evolved to survey and respond appropriately to the universe of foreign pathogens, deploying an intricate repertoire of mechanisms that keep responses to host tissues in check. The immune system is typically divided into two categories--innate and adaptive. Innate immunity refers to nonspecific defense mechanisms that come into play immediately or within hours of an antigen's appearance in the body. Adaptive immunity refers to antigen-specific immune response. The antigen first must be processed and recognized, and then the adaptive immune system creates an army of immune cells specifically designed to attack that antigen. For the adaptive immune system, specificity and sensitivity are provided by a large repertoire of antigen T-cell receptors (TCRs) constructed in their extracellular domain to recognize antigenic peptide fragments restricted and presented by histocompatibility complex molecules, and coupled through intracellular domains to signal transduction modules that serve to transmit environmental cues inside the cell.

Inflammation is triggered when innate immune cells detect infection or tissue injury. Pattern recognition receptors (PRRs) respond to pathogen-associated molecular patterns (PAMPs) or host-derived damage-associated molecular patterns (DAMPs) by triggering activation of NF-κB, AP1, CREB, c/EBP, and IRF transcription factors. Induction of genes encoding enzymes, chemokines, cytokines, adhesion molecules, and regulators of the extracellular matrix promotes the recruitment and activation of leukocytes. Besides resolving infection and injury, chronic inflammation is a risk factor for cancer.

Immunity has a major impact on inflammatory diseases and cancer, and biologics targeting immune cells and their factors. Immunosuppressant drugs suppress, or reduce, the strength of the body’s immune system, and have been used in the treatment of organ transplantation or autoimmunine diseases. Immunomodulator drugs have contributed to the significant improvement against cancer and other related diseases.

References:
[1] Sakaguchi S, et al. Immunol Cell Biol. 2012 Mar;90(3):277-87. doi: 10.1038/icb.2012.4.
[2] Newton K, et al. Cold Spring Harb Perspect Biol. 2012 Mar; 4(3): a006049.
[3] Bartneck M. Macromol Biosci. 2017 Apr 6. doi: 10.1002/mabi.201700021.


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STING agonist-20

STING agonist-20 (compound 95) is a potent STING agonist used in the synthesis of XMT-2056. STING agonist-20 can be used as a vaccine adjuvant in the study of cancer and other inflammatory, immune diseases[1].

  • CAS Number: 2591300-72-8
  • MF: C36H39N11O8
  • MW: 753.76
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sodium thiocyanate

Sodium thiocyanate reduces plasma levels of the pro-inflammatory cytokine IL-6, and increases the anti-inflammatory cytokine IL-10 levels. Sodium thiocyanate also significantly reduces of ROS formation[1].

  • CAS Number: 540-72-7
  • MF: CNNaS
  • MW: 81.072
  • Catalog: Interleukin Related
  • Density: 1.295 g/mL at 20 °C
  • Boiling Point: 146ºC at 760mmHg
  • Melting Point: 287 °C (dec.)(lit.)
  • Flash Point: 42.1ºC

Dectrekumab

Dectrekumab (QAX576) is a humanized monoclonal antibody that targets IL-13. Dectrekumab significantly improves intraepithelial esophageal eosinophil counts and dysregulated esophageal disease-related transcripts with Eosinophilic esophagitis (EoE) in a sustained manner and can be used for inflammation and immunology related research[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,3'-Diiodo-L-thyronine-13C6

3,3'-Diiodo-L-thyronine-13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine[1]. 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity[2][3].

  • CAS Number: 1217459-13-6
  • MF: C15H13I2NO4
  • MW: 531.03300
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Doxepin D3 Hydrochloride

Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant used as a sedative. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].

  • CAS Number: 347840-07-7
  • MF: C19H19D3ClNO
  • MW: 318.856
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: 64.0-65.0 °C at 760 mmHg
  • Melting Point: 162-164ºC
  • Flash Point: 9℃

Imiquimod (hydrochloride)

Imiquimod hydrochloride is an immune response modifier that acts as a toll-like receptor 7agonist.

  • CAS Number: 99011-78-6
  • MF: C14H17ClN4
  • MW: 276.76500
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CAY10621(SKI 5C)

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

  • CAS Number: 120005-55-2
  • MF: C26H45NO4
  • MW: 435.640
  • Catalog: SPHK
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 519.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 267.7±32.9 °C

Dostarlimab

Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

COX-2-IN-18

COX-2-IN-18 (Compound 3) is a potent inhibitor of COX-2. COX-2-IN-18 possesses good COX-2 inhibitory activity (IC50 = 0.775 μM) compared to the reference drug, Celecoxib (IC50 = 0.153 μM). COX-2-IN-18 has the potential for the research of cancer diseases[1].

  • CAS Number: 1038061-96-9
  • MF: C18H19N3O3S2
  • MW: 389.49
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Olamkicept

Olamkicept (FE 999301) is a selective inhibitor of the soluble interleukin 6 (sIL-6R)/IL-6 complex. Olamkicept is a soluble gp130-Fc-fusion-protein and anti-inflammatory agent[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(Rac)-γ-Tocopherol

(Rac)-γ-Tocopherol (DMPBQ) is a Vitamin E isoform, which is converted by tocopherol cyclase to γ-Tcopherol[1].

  • CAS Number: 73980-80-0
  • MF: C28H48O2
  • MW: 416.68
  • Catalog: COX
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 518.1±49.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 206.0±24.1 °C

Tagraxofusp

Tagraxofusp (SL-401) is a potent IL-3 receptor inhibitor to inhibits plasmacytoid dendritic cells (pDCs) growth in multiple myeloma (MM) bone marrow (BM) microenvironment. Tagraxofusp has synergistic effect with Bortezomib (HY-10227) and Pomalidomide (HY-10984) to suppress multiple myeloma (MM)[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cyclo(L-Phe-L-Pro)

Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide[1]. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation[2]. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay[3].

  • CAS Number: 3705-26-8
  • MF: C14H16N2O2
  • MW: 244.289
  • Catalog: Fungal
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 509.5±39.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 262.0±27.1 °C

Agatolimod sodium

Agatolimod sodium (ODN 7909) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’[1][2].

  • CAS Number: 541547-35-7
  • MF:
  • MW:
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Roburic Acid

Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively[1].

  • CAS Number: 6812-81-3
  • MF: C30H48O2
  • MW: 440.701
  • Catalog: COX
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 528.5±49.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 424.9±25.0 °C

Plozalizumab

Plozalizumab (MLN-1202) is a specific humanized anti-CCR2 antibody. Plozalizumab can be used for malignant melanoma research[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

COX-2-IN-11

COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PD-1/PD-L1-IN-21

PD-1/PD-L1-IN-21 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-21 blocks PD-1/PD-L1 with the IC50 of 4.99 μM. PD-1/PD-L1-IN-21 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].

  • CAS Number: 2158336-16-2
  • MF: C32H32BrClN2O4
  • MW: 623.96
  • Catalog: PD-1/PD-L1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(2S)-2-[methyl(prop-2-enoxycarbonyl)amino]propanoic acid

N-((Allyloxy)carbonyl)-N-methyl-L-alanine is a Alanine derivative. N-((Allyloxy)carbonyl)-N-methyl-L-alanine can be used for the synthesis of inhibitors of complement factor D. Complement factor D inhibitors can be used in the research of immune system related disease[1].

  • CAS Number: 918531-01-8
  • MF: C8H13NO4
  • MW: 187.19300
  • Catalog: Complement System
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCR2 antagonist 5

CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease[1].

  • CAS Number: 1228650-83-6
  • MF: C22H25F3N4O3S
  • MW: 482.51900
  • Catalog: CCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR7 agonist 8

TLR7 agonist 8 (compound IIb-34) is an TLR7 agonist with an EC50 value of ~4 nM[1].

  • CAS Number: 2380231-81-0
  • MF: C29H32N6O3
  • MW: 512.60
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-Catechin hydrate

(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. (±)-Catechin has two steric forms of (+)-Catechin and its enantiomer (-)-Catechin. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. Anticancer, anti-obesity, antidiabetic, anticardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects[1].

  • CAS Number: 7295-85-4
  • MF: C15H16O7
  • MW: 308.283
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: ~200 °C (dec.)
  • Flash Point: N/A

TLR8 agonist 2 hydrochloride

TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM)[1].

  • CAS Number: 2412937-65-4
  • MF: C16H22N8.xHCl
  • MW:
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

COX-1/2-IN-1

COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively[1].

  • CAS Number: 2358849-47-3
  • MF: C15H10BrClN2O
  • MW: 349.61
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Netakimab

Netakimab is an anti-IL-17 monoclonal antibody. Nerelimomab can be used for research of ankylosing spondylitis, psoriatic arthritis, moderate-to-severe plaque psoriasis[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hirsutal

Hirsutanonol ((5S)-Hirsutanonol) is a diarylheptanoid that can be isolated from the bark of Alnus hirsute var. sibirica. Hirsutanonol inhibits cyclooxygenase-2 (COX-2) expression. Hirsutanonol has anti-filarial with an IC50 value of 44.11 μg/mL for microfilariae[1].

  • CAS Number: 41137-86-4
  • MF: C19H22O6
  • MW: 346.374
  • Catalog: COX
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 679.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 378.8±28.0 °C

Amtolmetin guacil

Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2].

  • CAS Number: 87344-06-7
  • MF: C24H24N2O5
  • MW: 420.458
  • Catalog: Prostaglandin Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 663.3±55.0 °C at 760 mmHg
  • Melting Point: 117-120ºC
  • Flash Point: 354.9±31.5 °C

L6H21

L6H21, a derivative of chalcone, is an orally active and potent MD-2 (myeloid differentiation factor 2) inhibitor. L6H21 inhibits TLR4-NF-κB signaling and NLRP3 inflammasome activation in macrophages. L6H21 inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 effectively inhibits EtOH + LPS-induced hepatic fat accumulation and liver injury. L6H21 shows neuroprotective effect in a model of prediabetes[1][2].

  • CAS Number: 24533-47-9
  • MF: C18H18O4
  • MW: 298.33
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tesidolumab

Tesidolumab (LFG316) is a fully-human IgG1/λ anti-C5 monoclonal antibody of 143 kDa (without glycosylation). Tesidolumab (LFG316) blocks cleavage of C5 and prevents subsequent formation of the membrane attack complex[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-NIL dihydrochloride

L-NIL dihydrochloride is an inducible NO synthase inhibitor, with an IC50 of 3.3 μM for miNOS[1][2][3].

  • CAS Number: 159190-45-1
  • MF: C8H19Cl2N3O2
  • MW: 260.161
  • Catalog: NO Synthase
  • Density: N/A
  • Boiling Point: 369ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 177ºC