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1on itk Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Itk (15) Apoptosis (1) BCRP (1) BMX Kinase (1) Btk (7) CDK (1) EGFR (1) PARP (1) PROTACs (2) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (14) Inflammation/Immunology (11)

Inhibitors & Agonists

Peptides

Recombinant Proteins

Antibodies

Targets Recommended: Itk

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-125218

*PARP11 inhibitor ITK7* itk7	PARP	Cancer
PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC₅₀ value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization ^[1].

HY-13232

ITK antagonist	Itk	Inflammation/Immunology
ITK antagonist (compound 10 n) is a potent, orally active and selective *ITK* (Interleukin-2 inducible T-cell kinase) antagonist (IC₅₀=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC₅₀ of 160 nM ^[1].

HY-153322

ITK degrader 2

Itk Cancer

ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades ITK ^[1].
HY-146671

ITK inhibitor 5

Itk Cancer

ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC₅₀s of 5.6, 25 nM for ITK, BTK, respectively ^[1].

ITK degrader 2	Itk	Cancer
ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades *ITK* ^[1].

ITK inhibitor 5	Itk	Cancer
ITK inhibitor 5 (compound 27) is a potent and selective *ITK* inhibitor with IC₅₀s of 5.6, 25 nM for ITK, BTK, respectively ^[1].

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 ^[1].

HY-149917

ITK degrader 1	Itk	Cancer
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC₅₀=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC₅₀=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels ^[1].

HY-141864

ITK/TRKA-IN-1	Itk	Inflammation/Immunology
ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC₅₀ value of 1.0 nM and 96 % inhibition, respectively.

HY-128726

ITK inhibitor 2	Itk	Inflammation/Immunology
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC₅₀ of 2 nM.

HY-RS06979

ITK Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
ITK Human Pre-designed siRNA Set A contains three designed siRNAs for ITK gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

ITK Human Pre-designed siRNA Set A ITK Human Pre-designed siRNA Set A

HY-RS06980

Itk Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Itk Mouse Pre-designed siRNA Set A contains three designed siRNAs for Itk gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Itk Mouse Pre-designed siRNA Set A Itk Mouse Pre-designed siRNA Set A

HY-RS06981

Itk Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Itk Rat Pre-designed siRNA Set A contains three designed siRNAs for Itk gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Itk Rat Pre-designed siRNA Set A Itk Rat Pre-designed siRNA Set A

HY-130665

TL12-186 1 Publications Verification	PROTACs CDK	Cancer
TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, *ITK, et al. TL12-186 inhibits CDK2/cyclin A* (IC₅₀=73 nM) and CDK9/cyclin T1 (IC₅₀=55 nM) ^[1].

HY-109078

Vecabrutinib 2 Publications Verification SNS-062	Btk Itk	Cancer
Vecabrutinib (SNS-062) is a potent, noncovalent BTK and *ITK* inhibitor, with K_d values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC₅₀ of 24 nM for *ITK* ^[1] .

HY-108691

PF-06465469

Itk Cancer

PF-06465469 is a covalent inhibitor of ITK with an IC₅₀ of 2 nM ^[1].

PF-06465469	Itk	Cancer
PF-06465469 is a covalent inhibitor of *ITK* with an IC₅₀ of 2 nM ^[1].

HY-11092

BMS-509744 Maximum Cited Publications 6 Publications Verification	Itk	Inflammation/Immunology
BMS-509744 is a potent, selective and ATP competitive *Itk* inhibitor with an IC₅₀ of 19 nM.

HY-120559

GSK-2250665A

Itk Inflammation/Immunology

GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pK_i of 9.2.

GSK-2250665A	Itk	Inflammation/Immunology
GSK-2250665A (Compound 13) is a selective *Itk* inhibitor with a pK_i of 9.2.

HY-12680

PRN694 1 Publications Verification	Itk	Inflammation/Immunology
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC₅₀s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo ^[1].

HY-143900

BTK-IN-7	Btk Apoptosis	Inflammation/Immunology Cancer
BTK-IN-7 is a potent and selective inhibitor of BTK (IC₅₀=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity ^[1].

HY-150298

Soquelitinib CPI-818	Itk	Inflammation/Immunology Cancer
Soquelitinib (CPI-818) is a highlyl selective covalent *ITK* inhibitor. Soquelitinib decreases DNA replication and cell cycle signaling ^[1].

HY-143901

EGFR-IN-40

Btk EGFR Itk Cancer

EGFR-IN-40 (compound 3z) is a potent BTK, EGFR, and ITK inhibitor with IC₅₀ values of 1.2 nM, 5.3 nM, and 46.1 nM, respectively ^[1].

EGFR-IN-40	Btk EGFR Itk	Cancer
EGFR-IN-40 (compound 3z) is a potent BTK, EGFR, and *ITK* inhibitor with IC₅₀ values of 1.2 nM, 5.3 nM, and 46.1 nM, respectively ^[1].

HY-16984

GNE-4997
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity ^[1].

HY-12410

GNE-9822	Itk	Inflammation/Immunology
GNE-9822 is a potent, orally active and selective *ITK* inhibitor with a K_i value of 0.7 nM, and an EC₅₀ value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma ^[1] .

HY-110113

CTA056	Btk	Cancer
CTA056 is an *ITK* (IL-2-inducible T-cell kinase) inhibitor with an IC₅₀ of 0.1 μM. CTA056 selectively targets malignant T cells and modulates oncomirs. CTA056 induces apoptosis and is a potential therapeutic agent for the research of T-cell leukemia and lymphoma ^[1].

HY-145373

BMS-986143	Btk	Inflammation/Immunology
BMS-986143 is an orally active, reversible BTK inhibitor with an IC₅₀ of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC₅₀s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases ^[1].

HY-18010

PCI 29732 3 Publications Verification	Btk BCRP	Inflammation/Immunology
PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i ^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 ^[1] .

HY-80002

BMX-IN-1 4 Publications Verification BMX kinase inhibitor	Btk BMX Kinase	Cancer
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys ⁴⁹⁶ in the BMX ATP binding domain with an IC₅₀ of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC₅₀ value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

HY-148065

FMF-06-098-1	PROTACs	Cancer
FMF-06-098-1 is a multitargeted depressant. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 ^[1].

Srctide	Peptides	Others
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)

Species:	Human (2) Mouse (1)
Tag:	His (1) GST (3)
Source:	Sf9 insect cells (3)

Cat. No.	Compare	Product Name	Species	Source

HY-P74796

	ITK Protein, Human (sf9, GST) Tyrosine-protein kinase itk/TSK; IL-2-inducible T-cell kinase; itk; EMT; LYK	Human	Sf9 insect cells
	ITK protein is an important tyrosine kinase that regulates adaptive immune responses by affecting the development and function of T cells and NKT cells. Upon T cell receptor (TCR) activation, ITK undergoes LCK-mediated phosphorylation, leading to its activation. ITK Protein, Human (sf9, GST) is the recombinant human-derived ITK protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of ITK Protein, Human (sf9, GST) is 269 a.a., with molecular weight of ~57.7 kDa.

HY-P74795

	ITK Protein, Mouse (sf9, His-GST) Tyrosine-protein kinase itk/TSK; IL-2-inducible T-cell kinase; itk; EMT; LYK	Mouse	Sf9 insect cells
	ITK protein is a tyrosine kinase that plays a crucial role in directing adaptive immune responses by controlling the development, function, and differentiation of conventional T cells and unconventional NKT cells. After T cell receptor (TCR) activation by antigen-presenting cells (APC), ITK is recruited to the cell membrane and phosphorylated by LCK, thereby making it fully activated. ITK Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived ITK protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of ITK Protein, Mouse (sf9, His-GST) is 269 a.a., with molecular weight of ~58 kDa.

HY-P702731

	ITK Protein, Human (620a.a, sf9, GST) itk; IL2-inducible T-cell kinase; tyrosine-protein kinase itk/TSK; EMT; LYK; PSCTK2; kinase EMT; T-cell-specific kinase; tyrosine-protein kinase LYK; IL-2-inducible T cell kinase; IL-2-inducible T-cell kinase; homolog of mouse T-cell itk/tsk; interleukin-2-inducible T cell kinase; interleukin-2-inducible T-cell kinase; MGC126257; MGC126258	Human	Sf9 insect cells


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