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.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
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Immunology/Inflammation >
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JAK/STAT Signaling >
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ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
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Vitamin D Related >
VD/VDR
Others >
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Phenethyl ferulate

Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].

  • CAS Number: 71835-85-3
  • MF: C18H18O4
  • MW: 298.33
  • Catalog: COX
  • Density: 1.193g/cm3
  • Boiling Point: 474.7ºC at 760 mmHg
  • Melting Point: 81℃
  • Flash Point: 171.6ºC

Methyl Salicylate-d4

Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].

  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 222.0±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 86.8±12.6 °C

Salicylic acid-D6

Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation[1].

  • CAS Number: 285979-87-5
  • MF: C7D6O3
  • MW: 138.121
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 336.3±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 144.5±19.1 °C

diABZI STING agonist-1 (Tautomerism)

diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.

  • CAS Number: 2138498-18-5
  • MF: C42H51N13O7
  • MW: 849.94
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-(-)-α-Methylhistamine dihydrochloride

(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats[3][4][5].

  • CAS Number: 75614-89-0
  • MF: C6H13Cl2N3
  • MW: 198.09400
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TLR7-Agonist-31

A potent TLR7 agonist with EC50 of 59 nM.

  • CAS Number: 1229024-57-0
  • MF: C21H22N4
  • MW: 330.435
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JAK2/STAT3-IN-1

JAK2/STAT3-IN-1 (compound (S)-10a) is a potent GP130 inhibitor with an IC50 of 3.04 µM. JAK2/STAT3-IN-1 shows anti-tumor activity[1].

  • CAS Number: 2485758-50-5
  • MF: C34H35BrF3N5O2
  • MW: 682.57
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMD-070

AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.

  • CAS Number: 558447-26-0
  • MF: C21H27N5
  • MW: 349.473
  • Catalog: HIV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 597.0±50.0 °C at 760 mmHg
  • Melting Point: 108-110ºC
  • Flash Point: 314.9±30.1 °C

3-Phenoxybenzaldehyde

3-Phenoxybenzaldehyde has weak complement classical pathway inhibition and hemolytic activity[1].

  • CAS Number: 39515-51-0
  • MF: C13H10O2
  • MW: 198.22
  • Catalog: Complement System
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 392.4±0.0 °C at 760 mmHg
  • Melting Point: 13 °C
  • Flash Point: 156.1±13.9 °C

(±)-Tazifylline

(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.

  • CAS Number: 79712-55-3
  • MF: C23H32N6O3S
  • MW: 472.60400
  • Catalog: Histamine Receptor
  • Density: 1.34g/cm3
  • Boiling Point: 705.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 380.2ºC

Dehydroglyasperin D

Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi[1][2][3].

  • CAS Number: 517885-72-2
  • MF: C22H24O5
  • MW: 368.42
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 557.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 291.2±30.1 °C

MyD88-IN-1

MyD88-IN-1 is a potent MyD88 inhibitor. MyD88-IN-1 inhibits the interaction of TLR4 and MyD88 and suppressed the NF-κB pathway. MyD88-IN-1 can be used in research of cancer and inflammatory[1].

  • CAS Number: 2911609-80-6
  • MF: C23H24N6O7S
  • MW: 528.54
  • Catalog: MyD88
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mavacoxib

Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs[1].

  • CAS Number: 170569-88-7
  • MF: C16H11F4N3O2S
  • MW: 385.336
  • Catalog: COX
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 519.8±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 268.2±32.9 °C

KTX-497

KTX-497 is an orally active IRAK4 degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology[1].

  • CAS Number: 2432993-46-7
  • MF: C45H49F3N8O6
  • MW: 854.92
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Prifelone

Prifelone (R 830; R 830T; S 16820) is a di-tert-butylphenol with anti-inflammatory and antioxidant activity. Prifelone inhibits guinea pig lung oxygenase and bovine seminal vesicle cyclooxygenase[1].

  • CAS Number: 69425-13-4
  • MF: C19H24O2S
  • MW: 316.45800
  • Catalog: COX
  • Density: 1.095g/cm3
  • Boiling Point: 422ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 209ºC

Cinnarizine D8

Cinnarizine D8 is a deuterium labeled Cinnarizine. Cinnarizine is an antihistamine and a calcium channel blocker.

  • CAS Number: 1185242-27-6
  • MF: C26H20D8N2
  • MW: 376.56300
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NFAT Transcription Factor Regulator

NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.

  • CAS Number: 245747-71-1
  • MF: C17H10F6N4O2
  • MW: 416.28
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CHD-5

CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist[1].

  • CAS Number: 289494-16-2
  • MF: C19H17N3O2
  • MW: 319.357
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 426.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.0±28.7 °C

GSK717

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].

  • CAS Number: 1595278-21-9
  • MF: C28H28N4O2
  • MW: 452.55
  • Catalog: NOD-like Receptor (NLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromfenac-d4 sodium

Bromfenac-d4 (sodium) is deuterium labeled Bromfenac (sodium). Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME)[1][2].

  • CAS Number: 2749400-35-7
  • MF: C15H7D4BrNNaO3
  • MW: 360.17
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ATI-2341 TFA

ATI-2341 is a CXCR4 agonist, induces CXCR4-dependent calcium flux, with an EC50 of 194 nM in CCRF-CEM cells. ATI-2341 is also a potent and efficacious mobilizer of bone marrow hematopoietic cells[1].

  • CAS Number: 1337878-62-2
  • MF: C104H178N26O25S2
  • MW: 2256.82
  • Catalog: CXCR
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lck Inhibitor III

Lck Inhibitor III (compound 12h) is a potent Lck inhibitor, with an IC50 of 867 nM. Lck Inhibitor III inhibits IL-2 synthesis in Jurkat cells, with an IC50 of 1.270 μM[1].

  • CAS Number: 1188890-30-3
  • MF: C25H28N6O3・H2O
  • MW: 478.55
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mercaptoethylguanidine (MEG) (dihydrobromide)

Mercaptoethylguanidine (MEG) dihydrobromide is selective inhibitor of the inducible nitric oxide synthase and peroxynitrite scavenger. Mercaptoethylguanidine (MEG) dihydrobromide has the potential for inflammatory bowel diseases research.

  • CAS Number: 32665-11-5
  • MF: C3H10BrN3S
  • MW: 200.10100
  • Catalog: NO Synthase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CXCR4 antagonist 9

CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM[1].

  • CAS Number: 2304750-83-0
  • MF: C21H27FN6
  • MW: 382.48
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MSX-130

MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis[1].

  • CAS Number: 4051-59-6
  • MF: C36H26N4
  • MW: 514.618
  • Catalog: CXCR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 766.3±48.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 326.5±22.5 °C

Setastine

Setastine (EGIS-2062 (free acid); EGYT-2062 (free acid) is an orally effective, non-sedative and long acting anti-allergic agent. Setastine possesses potent histamine Hi-receptor blocking properties and can be used for allergies and rhinitis research[1]<.

  • CAS Number: 64294-95-7
  • MF: C22H28ClNO
  • MW: 357.91700
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

elsilimomab

Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA)[1][2][3].

  • CAS Number: 468715-71-1
  • MF:
  • MW:
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cogentin

Benztropine mesylate is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research[1]. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2].

  • CAS Number: 86-13-5
  • MF: C21H25NO
  • MW: 307.42900
  • Catalog: Dopamine Receptor
  • Density: 1.11g/cm3
  • Boiling Point: 409ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 120.1ºC

L-Lysine6-13C dihydrochloride

L-Lysine6-13C (dihydrochloride) is a 13C-labeled Sulfamethoxypyridazine.

  • CAS Number: 1217466-44-8
  • MF: C513CH16Cl2N2O2
  • MW: 220.10
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CU-CPT-8m

CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.

  • CAS Number: 125079-83-6
  • MF: C14H12N4O
  • MW: 252.27
  • Catalog: Toll-like Receptor (TLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A