Epacadostat (INCB024360)
CAS 1204669-58-8
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
Immunology & Inflammation
Innate and adaptive immunity, inflammatory pathways and immune signaling.
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LFM-A13
CAS 244240-24-2
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
R406 free base
CAS 841290-80-0
R406 is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.
CEP33779
CAS 1257704-57-6
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
Indirubin
CAS 479-41-4
Indirubin(Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.IC50 value:Target:in vitro: The activation of EGF receptor, known to be highly expressed…
Balixafortide(POL6326)
CAS 1051366-32-5
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and…
LY2409881 trihydrochloride
CAS 946518-60-1
LY2409881 trihydrochloride is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
RIP1 inhibitor GSK547
CAS 2226735-55-1
GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
SN-011
CAS 2249435-90-1
STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-mediated disease.
GW-627368X
CAS 439288-66-1
GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors…
INCB024360 analogue(IDO-IN-1)
CAS 914471-09-3
IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM.
BLZ-945
CAS 953769-46-5
BLZ945 is a potent, selective and brain-penetrant CSF-1R inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
Eupatilin
CAS 22368-21-4
Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
Indoximod (NLG-8189)
CAS 110117-83-4
Indoximod (D-1MT, NLG8189) is an indoleamine 2,3-dioxygenase (IDO) pathway inhibitor with a Ki of 19 μM.
Fingolimod HCl（FTY-720）
CAS 162359-56-0
Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells.
CWHM-12
CAS 1564286-55-0
CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
Apremilast
CAS 608141-41-9
Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM.
Plerixafor octahydrochloride
CAS 155148-31-5
Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
GSK2981278
CAS 1474110-21-8
GSK2981278 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124.
Taprenepag(CP-544326)
CAS 752187-80-7
CP-544326 is a potent and selective prostaglandin E2 receptor agonist with an EC50 of 2.8 nM.
Crisaborole(AN-2728)
CAS 906673-24-3
AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines. AN-2728 appears to have good therapeutic potential, although…
BAF312 (Siponimod)
CAS 1230487-00-9
Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively.)
LIT927
CAS 2172879-52-4
LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding.
Ivacaftor (VX-770)
CAS 873054-44-5
Ivacaftor is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
XL019
CAS 945755-56-6
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with good selectivity against the Janus Kinase family as well as a broad kinase panel.XL019 was…
Olodaterol(BI-1744) hydrochloride
CAS 869477-96-3
Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary…
Sivelestat (sodium salt hydrate)
CAS 201677-61-4
Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma…
Acalabrutinib(ACP196)
CAS 1420477-60-6
Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
TG100-115
CAS 677297-51-7
TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
PD-1/PD-L1 inhibitor 2(BMS-202)
CAS 1675203-84-5
BMS-202 is an inhibitor of the PD-1/PD-L1 protein/protein interaction with an IC50 of 18 nM.
IMD-0354
CAS 978-62-1
IMD-0354 is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM.
S-Ruxolitinib (INCB018424)
CAS 941685-37-6
INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424 (64 nM) results in a doubling of cells
Apilimod mesylate
CAS 870087-36-8
Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-γ/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.
ITF2357
CAS 199657-29-9
Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride.…
Edicotinib（JNJ-40346527）
CAS 1142363-52-7
Edicotinib（JNJ-40346527）is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between…
Ozanimod (RPC1063)
CAS 1306760-87-1
Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively.
Ki20227
CAS 623142-96-1
Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.IC50 value: Target: CSF1Rin vitro: Ki20227 did not inhibit…
Evobrutinib
CAS 1415823-73-2
Evobrutinib is an inhibitor of Bruton's tyrosin kinase (Btk) inhibitor extracted from patent US20140162983 example 0174.
BMS-986020
CAS 1257213-50-5
BMS-986020 is an LPA1 antagonist.target: LPA1BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic…
E-7046
CAS 1369489-71-3
E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
E6005
CAS 947620-48-6
Lotamilast is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM..
Ascomycin (Immunomycin,FK-520)
CAS 104987-12-4
Ascomycin(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.
Pexidartinib(PLX3397)
CAS 1029044-16-3
Pexidartinib (PLX-3397) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13 nM, 27 nM, and 11 nM for CSF1R, c-Kit, and FLT3, respectively.
NIBR189
CAS 1599432-08-2
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).NIBR189 is a potent and selective EBI2 antagonist with improved pharmacokinetic properties which will…
MSX-122
CAS 897657-95-3
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
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