DC71796 |
IST5-002 |
IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML). |
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DC72042 |
SJ1008030 |
SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cells with an EC50 of 5.4 nM and an IC50 of 32.09 nM. SJ1008030 can be used for the research of leukemia. |
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DC72043 |
VVD-118313
Featured
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VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. |
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DC72044 |
Peficitinib hydrochloride |
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. |
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DC72045 |
(S)-PM-43I |
(S)-PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. (S)-PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research[1]. |
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DC72046 |
PM-81I |
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1]. |
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DC72210 |
NDI-034858(Zasocitinib)
Featured
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NDI034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. |
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DC72211 |
HP590 |
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis. |
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DC72355 |
STX-0119 |
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM. |
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DC72356 |
GYY4137 |
GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity. |
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DC72357 |
inS3-54-A18 |
inS3-54A18 is a potent inhibitor of STAT3 with anti-cancer properties. |
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DC72649 |
Nimucitinib
Featured
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Nimucitinib is a Janus kinase (JAK) inhibitor. |
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DC72650 |
Pumecitinib |
Pumecitinib is a Janus kinase (JAK) inhibitor with anti-inflammatory activity. |
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DC73567 |
ABBV-712 |
ABBV-712 is a potent, selective inhibitor of tyrosine kinase 2 (TYK2) with EC50 of 0.01 uM, binds and stabilizes the pseudokinase (JH2) domain of TYK2. |
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DC73568 |
ABT-317 |
ABT-317 (ABT317) is a potent, selective JAK1 inhibitor, inhibits IL-6-stimulated pSTAT3 (TF-1 cells, IC50=16 nM) and IL-2-stimulated pSTAT5 (T-blasts, IC50=30 nM). |
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DC73569 |
ATI-1777 |
ATI-1777 is a potent, selective and ATP-competitive JAK1/3 inhibitor with IC50 of 1.5/3.6/7.1/19.0 nM for JAK1/JAK2/JAK3/TYK2, respectively. |
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DC73570 |
AZD0449 |
AZD0449 (AZD-0449) is a potent and highly selective JAK1 inhibitor with IC50 of 2.4 nM, displays >50-fold selectivity over TYK2 and JAK2, and no inhibition against JAK3. |
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DC73571 |
CPL409116 |
CPL409116 (CPL 409116) is a potent, competitive, dual JAK and ROCK inhibitor with IC50 of 0.95/5.36//0.87/110.6/106.7 nM for JAK1/JAK2/JAK3/ROCK1/ROCK2, respectively. |
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DC73572 |
MMT3-72 |
MMT3-72 is a gastrointestinal locally-activating Janus kinase (JAK) inhibitor, readily converted to MMT3-72-M2 in the colon contents (JAK1 IC50=10.8 nM, JAK2 IC50=26.3 nM and TYK2 IC50=91.6 nM). |
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DC73573 |
QL-1200186 |
QL-1200186 is a potent, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 0.06 nM, targets pseudokinase regulatory domain (Janus homology 2, JH2) of the TYK2 protein. |
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DC73574 |
Ruxolitinib sulfate |
A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively. |
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DC73575 |
YLIU-5-162-1 |
YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib. |
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DC73576 |
Z583 |
Z583 is a potent, highly selective JAK3 inhibitor with IC50 of 0.1 nM, 4500-fold selectivity over other JAK subtypes. |
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DC73577 |
DR-1-55 |
DR-1-55 (DR-155) is a selective STAT3 inhibitor that covalently modifies a cysteine in the SH2 domain of STAT3. |
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DC73578 |
K1836 |
K1836 is a small molecule Stattic analog inhibitor of STAT3 signalling. |
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DC73579 |
LLL12B |
LLL12B is a selective STAT3 inhibitor that suppresses Th17 development, specifically inhibits STAT3 and suppresses Th17 differentiation and expansion. |
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DC73580 |
MC0704 |
MC0704 (MC-0704) is a novel synthetic STAT3 pathway inhibitor, exhibits potential antitumor activity in vitro and in vivo models in docetaxel-resistant TNBC cells. |
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DC73581 |
MNS1-Leu |
MNS1-Leu is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells. |
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DC73582 |
MNS1-MV |
MNS1-MV is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells. |
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DC73583 |
ODZ10117 |
ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines. |
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