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Results for "

phosphorylation JAK3

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) Atg8/LC3 (3) Autophagy (3) Bcl-2 Family (1) Caspase (3) EGFR (1) Interleukin Related (4) Isotope-Labeled Compounds (1) Itk (1) JAK (18) JNK (1) NF-κB (1) p62 (3) PARP (1) PERK (1) Reactive Oxygen Species (ROS) (3) STAT (10)
By Research Areas:	Cancer (15) Cardiovascular Disease (3) Inflammation/Immunology (11)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Targets Recommended: Oxidative Phosphorylation DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100754C

Ritlecitinib tosylate Maximum Cited Publications 9 Publications Verification PF-06651600 tosylate	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent *JAK3* inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-100754

Ritlecitinib Maximum Cited Publications 9 Publications Verification PF-06651600	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent *JAK3* inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-116505

JAK1-IN-4	JAK	Cancer
JAK1-IN-4 is a potent and selective *JAK1* inhibitor, with IC₅₀s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC₅₀, 227 nM) .

HY-111553

TAS0728	EGFR	Cancer
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for *BMX、HER4、BLK、EGFR、JAK3、SLK* and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors .

HY-P5434

Jak3tide JAK3 Peptide substrate	JAK	Others
Jak3tide (JAK3 Peptide substrate) is a biological active peptide. (This peptide is a substrate for Jak3. It may be used used in kinase assays. Jak3tide contains the phosphorylation site at Tyr7.)

HY-121874

EP009	JAK	Cancer
EP009 is a *JAK3* inhibitor that selectively inhibits IL-2-mediated *JAK3* tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .

HY-100754A

Ritlecitinib (malonate) PF-06651600 (malonate)	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent *JAK3* inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-168339

Tyk2-IN-22	JAK	Inflammation/Immunology
Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .

HY-146672

ITK inhibitor 6	Itk	Cancer
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC₅₀s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .

HY-153702

JAK-IN-27	JAK	Cancer
JAK-IN-27 (compound 1) is an orally active and potent *JAKS* family kinase inhibitor with IC₅₀s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC₅₀=23.7 nM) .

HY-112724A

Ivarmacitinib sulfate SHR0302 sulfate	JAK Apoptosis	Inflammation/Immunology Cancer
Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly *JAK1. The selectivity of Ivarmacitinib for JAK1* is >10-fold for *JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3* phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .

HY-112724

Ivarmacitinib SHR0302	JAK Apoptosis	Inflammation/Immunology Cancer
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly *JAK1. The selectivity of Ivarmacitinib for JAK1* is >10-fold for *JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3* phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .

HY-120604

BVB808 NVP_BVB808	JAK STAT	Cancer
BVB808 (NVP_BVB808) is a selective *JAK2* inhibitor with approximately 10-fold selectivity for *JAK2* over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of *JAK2* and reduces the phosphorylation of STAT5, thereby blocking the *JAK2*-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research .

HY-169984S

Tyk2-IN-22-d3	Isotope-Labeled Compounds STAT JAK	Inflammation/Immunology
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .

HY-13775

XL019 5+ Cited Publications	JAK Apoptosis	Cancer
XL019?is a potent, orally active, and selective *JAK2* inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .

HY-111077

INCB16562	JAK STAT	Inflammation/Immunology Cancer
INCB16562 is an orally active and selective inhibitor against *JAK1/2* markedly selective over *JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation* of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .

HY-170927

JAK-IN-40	JAK STAT Apoptosis	Cancer
JAK-IN-40 (Compound 46) is the inhibitor for *JAK* that inhibits *JAK1, JAK2* and *JAK3* with IC₅₀s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI₅₀ of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .

HY-13559A

Atiprimod dimaleate Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate	STAT Apoptosis Caspase Interleukin Related Autophagy Reactive Oxygen Species (ROS) Atg8/LC3 p62 JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the *JAK-STAT* signaling pathway by inhibiting the phosphorylation of *JAK2* and *JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy* and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-13559

Atiprimod Azaspirane ; SKF 106615-12; SKF 106615A12	STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family p62 Atg8/LC3 PARP NF-κB PERK JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the *JAK-STAT* signaling pathway by inhibiting the phosphorylation of *JAK2* and *JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy* and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-110102

Atiprimod hydrochloride Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615	JAK STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Atg8/LC3 p62	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the *JAK-STAT* signaling pathway by inhibiting the phosphorylation of *JAK2* and *JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy* and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-150688

JAK3-IN-13	JNK	Cancer
JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC₅₀ values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .

Cat. No.	Product Name	Target	Research Area

HY-P5434

Jak3tide JAK3 Peptide substrate	JAK	Others
Jak3tide (JAK3 Peptide substrate) is a biological active peptide. (This peptide is a substrate for Jak3. It may be used used in kinase assays. Jak3tide contains the phosphorylation site at Tyr7.)

Cat. No.	Product Name	Chemical Structure

HY-169984S

Tyk2-IN-22-d3
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .

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