Immunology & Inflammation

MI 2 (MALT1 inhibitor)

CAS 1047953-91-2

MI 2 (MALT1 inhibitor) is an irreversible MALT1 protease inhibitor with an IC50 of 5.84 μM.

TG6-10-1

CAS 1415716-58-3

TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.

YM 90709

CAS 163769-88-8

YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor.

Solcitinib（GLPG0778）

CAS 1206163-45-2

Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.

WHI-P258

CAS 21561-09-1

WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].

R788 disodium (Fostamatinib)

CAS 1025687-58-4

Fostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

GSK2982772

CAS 1622848-92-3

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.

Bay 11-7085

CAS 196309-76-9

BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.

SC-514 (GK 01140)

CAS 354812-17-2

SC-514 is a selective IKK-2 inhibitor (IC50=11.2±4.7 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

Upadacitinib

CAS 1310726-60-3

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.

RS 504393

CAS 300816-15-3

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

Sarecycline(P005672 hydrochloride)

CAS 1035979-44-2

Sarecycline hydrochloride is a narrow-spectrum tetracycline-class antibiotic. Sarecycline hydrochloride possesses anti-inflammatory properties and potent activity against Gram-positive bacteria, including activity against multiple strains of Cutibacterium…

Emricasan

CAS 254750-02-2

Emricasan (PF 03491390) is an irreversible pan-caspase inhibitor.

STING agonist-1 trihydrochloride

CAS 2138299-34-8

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist.

Lodoxamide

CAS 53882-12-5

Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.

MSA-2

CAS 129425-81-6

MSA-2 is an orally available non-nucleotide STING agonist, with EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable…

Inarigivir(ORI-9020,SB-9000)

CAS 475650-36-3

Inarigivir (ORI-9020;SB-9000) is a dinucleotide which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus.

SC75741

CAS 913822-46-5

SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of…

FM-381

CAS 2226521-65-7

FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.

PF-06651600

CAS 1792180-81-4

PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.

PD-1-IN-17(CA-170)

CAS 1673560-66-1

PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].

NS-398

CAS 123653-11-2

NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.

Parthenolide

CAS 20554-84-1

Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.

Triptolide

CAS 38748-32-2

Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.

Bepotastine Besilate

CAS 190786-44-8

Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.

INF39

CAS 866028-26-4

INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.

NOD-IN-1

CAS 132819-92-2

NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.

IKK(epsilon)-IN-1 (IKKE-IN-1)

CAS 1292310-49-6

TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.

IKK-16(free base)

CAS 873225-46-8

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

AZD2098

CAS 566203-88-1

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.

Fevipiprant

CAS 872365-14-5

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human…

CU-CPT-9b

CAS 2162962-69-6

CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM.

N6022

CAS 1208315-24-5

N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor with IC50 of 8 nM.

SC-26196

CAS 218136-59-5

SC-26196 is a potent, orally active Delta6 desaturase (D6D) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties[1].

BGB-3111(Zanubrutinib)

CAS 1691249-45-2

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

MRE-269

CAS 475085-57-5

MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.

Cyclic-di-GMP(c-di-GMP)

CAS 61093-23-0

Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.

Peficitinib（ASP015K,JNJ-54781532）

CAS 944118-01-8

Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

GLPG-1690(Ziritaxestat)

CAS 1628260-79-6

GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.

PSB-16671

CAS 2094630-35-8

PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of…

NLG919(GDC-0919)

CAS 1402836-58-1

IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.

GSK-805

CAS 1426802-50-7

GSK805, also known as ROR gamma-t-IN-1, is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.

QNZ(EVP4593)

CAS 545380-34-5

QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.

Icatibant

CAS 130308-48-4

Icatibant is a peptidomimetic drug consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It has been approved by the European Commission for the symptomatic treatment of acute attacks of hereditary angioedema…

DMXAA

CAS 117570-53-3

Vadimezan (ASA-404; DMXAA), the vascular disrupting agent, is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.

Pizuglanstat

CAS 1244967-98-3

Pizuglanstat is a potent, selective prostaglandin D synthase inhibitor.

MKK7-COV-3

MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without…

AZD1981

CAS 802904-66-1

AZD1981 is a potent and selective CRTh2 antagonist; displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).