Search Result

Results for "

BCR-ABL

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bcr-Abl (101) Ack1 (1) Akt (1) Antibiotic (1) Apoptosis (25) Aurora Kinase (3) Autophagy (22) Bacterial (1) Bcl-2 Family (1) c-Kit (13) c-Myc (1) Casein Kinase (1) CRISPR/Cas9 (1) Deubiquitinase (1) Drug Metabolite (5) E3 Ligase Ligand-Linker Conjugates (1) EGFR (1) FLT3 (4) HDAC (2) Histone Methyltransferase (1) IGF-1R (2) Insulin Receptor (1) Isotope-Labeled Compounds (3) JAK (4) Ligands for E3 Ligase (3) Microtubule/Tubulin (1) p38 MAPK (1) PDGFR (15) PROTACs (6) SARS-CoV (6) SNIPERs (12) Src (11) STAT (2) Thymidylate Synthase (1) Tyrosinase (1)
By Research Areas:	Cancer (112) Cardiovascular Disease (1) Endocrinology (2) Infection (1) Inflammation/Immunology (3) Neurological Disease (2)

By Targets:

Bcr-Abl (101)

Ack1 (1)

Akt (1)

Antibiotic (1)

Apoptosis (25)

Aurora Kinase (3)

Autophagy (22)

Bacterial (1)

Bcl-2 Family (1)

c-Kit (13)

c-Myc (1)

Casein Kinase (1)

CRISPR/Cas9 (1)

Deubiquitinase (1)

Drug Metabolite (5)

E3 Ligase Ligand-Linker Conjugates (1)

EGFR (1)

FLT3 (4)

HDAC (2)

Histone Methyltransferase (1)

IGF-1R (2)

Insulin Receptor (1)

Isotope-Labeled Compounds (3)

JAK (4)

Ligands for E3 Ligase (3)

Microtubule/Tubulin (1)

p38 MAPK (1)

PDGFR (15)

PROTACs (6)

SARS-CoV (6)

SNIPERs (12)

Src (11)

STAT (2)

Thymidylate Synthase (1)

Tyrosinase (1)

By Research Areas:

Cancer (112)

Cardiovascular Disease (1)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (3)

Neurological Disease (2)

117

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Bcr-Abl

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156148

BCR-ABL-IN-8	Bcr-Abl	Cancer
BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group .

HY-160174

BCR-ABL kinase-IN-3	Bcr-Abl	Cancer
BCR-ABL kinase-IN-3 (example 1) is a potent inhibitor of *BCR-ABL* that plays an important role in acute myeloid leukemia (AML) research .

HY-160174A

BCR-ABL kinase-IN-3 (dihydrocholide)	Bcr-Abl	Cancer
BCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of *BCR-ABL* that plays an important role in acute myeloid leukemia (AML) research .

HY-150566

BCR-ABL-IN-5	Bcr-Abl	Cancer
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl ^WT and Bcr-Abl ^T3151 with the IC₅₀ value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .

HY-142922

BCR-ABL-IN-4	Bcr-Abl	Cancer
BCR-ABL-IN-4 is a *BCR-ABL* inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC₅₀ values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .

HY-169231

BCR-ABL-IN-10	Bcr-Abl	Cancer
BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing *BCR-ABL* inhibitor with an IC₅₀ of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML) .

HY-136526

BCR-ABL-IN-3	Bcr-Abl	Cancer
BCR-ABL-IN-3 is a potent and irreversible *Bcr-Abl* inhibitor with an IC₅₀ of ≤100 nM for Ba/F₃Bcr-Abl ^T3151. BCR-ABL-IN-3 has anti-cancer activity .

HY-150569

BCR-ABL-IN-6	Bcr-Abl	Cancer
BCR-ABL-IN-6 (9h) is a selective *Bcr-Abl* kinase inhibitor with IC₅₀s of 4.6 and 227 nM for Bcr-Abl ^WT and Bcr-Abl ^T3151 respectively. BCR-ABL-IN-6 inhibits *Bcr-Abl* kinase with strong affinity inside the cells with an EC₅₀ of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia . BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-169230

BCR-ABL-IN-9	Bcr-Abl	Cancer
BCR-ABL-IN-9 (Compound B1) is a *BCR-ABL* inhibitor that achieves sustained *BCR-ABL* suppression by forming stable covalent bonds with the ABL kinase. BCR-ABL-IN-9 is also effective in inhibiting the activity of the ABL kinase (IC₅₀ = 1.2 nM). BCR-ABL-IN-9 possesses anticancer activity .

HY-100314

BCR-ABL-IN-1	Bcr-Abl	Cancer
BCR-ABL-IN-1 is an inhibitor of *BCR-ABL* tyrosine kinase, with a pIC₅₀ of 6.46, and may be used in the research of chronic myelogenous leukemia.

HY-145887

BCR-ABL1-IN-1	Bcr-Abl	Neurological Disease
BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABL kinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABL kinases in the brain in non-clinical studies .

HY-18819

BCR-ABL-IN-2	Bcr-Abl	Cancer
BCR-ABL-IN-2 is an inhibitor of *BCR-ABL1* tyrosine kinase, with IC₅₀s of 57 nM, 773 nm for ABL1 ^native and ABL1 ^T315I, respectively.

HY-153008

BCR-ABL-IN-7	Bcr-Abl	Cancer
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research .

HY-153415

*PROTAC BCR-ABL* Degrader-1**	PROTACs Bcr-Abl	Cancer
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces *Bcr-Abl* degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .

HY-130297

*PROTAC BCR-ABL1 ligand 1*	Bcr-Abl	Cancer
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets *BCR-ABL1* protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1 .

HY-162952

*cSRC/BCR-ABL1-IN-1*	Bcr-Abl	Cancer
cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target *cSRC/BCR-ABL1* kinase inhibitor .

HY-157327

AKE-72	Bcr-Abl	Cancer
AKE-72 (compound 5) is a potent inhibitor of *Pan-BCR-ABL. AKE-72 inhibits BCR-ABL* ^WT, BCR-ABL ^T315, BCR-ABL ^E255K, BCR-ABL ^F3171, BCR-ABL ^H396P and BCR-ABL ^Q252H with IC₅₀s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line .

HY-10159A

Nilotinib monohydrochloride monohydrate 30+ Cited Publications AMN107 monohydrochloride monohydrate	Bcr-Abl Autophagy	Cancer
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against *BCR-ABL, and is active against many BCR-ABL* mutants.

HY-10159AR

Nilotinib monohydrochloride monohydrate (Standard)	Bcr-Abl Autophagy	Cancer
Nilotinib (monohydrochloride monohydrate) (Standard) is the analytical standard of Nilotinib (monohydrochloride monohydrate). This product is intended for research and analytical applications. Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against *BCR-ABL, and is active against many BCR-ABL* mutants.

HY-10159

Nilotinib 30+ Cited Publications AMN107	Bcr-Abl Autophagy	Cancer
Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-15666

Olverembatinib 5 Publications Verification GZD824; HQP1351	Bcr-Abl	Cancer
Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl ^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10159S

Nilotinib-d6 AMN107-d₆	Bcr-Abl Autophagy	Cancer
Nilotinib-d₆ is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].

HY-15666A

Olverembatinib dimesylate 5 Publications Verification GZD824 dimesylate; HQP1351 dimesylate	Bcr-Abl	Cancer
Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl ^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity . Olverembatinib (dimesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15666R

Olverembatinib (Standard)	Bcr-Abl	Cancer
Olverembatinib (Standard) is the analytical standard of Olverembatinib. This product is intended for research and analytical applications. Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl ^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15493

AN-019 NRC-AN-019	Bcr-Abl	Cancer
AN-019 is a *Bcr-Abl* kinase inhibitor. AN-019 has antitumor activity .

HY-10159R

Nilotinib (Standard)	Bcr-Abl Autophagy	Cancer
Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-10159B

Nilotinib hydrochloride AMN107 hydrochloride	Bcr-Abl Autophagy	Cancer
Nilotinib (AMN107) hydrochloride is an orally active *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia .

HY-119177

PD173956	Bcr-Abl	Others
PD173956 is a pyridopyrimidine Bcr-Abl kinase inhibitor with high selectivity for the P-loop mutant form of Bcr-Abl .

HY-101489

GZD856	PDGFR Bcr-Abl Apoptosis	Cancer
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC₅₀s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl ^T315I inhibitor, with IC₅₀s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity .

HY-153582

ML 2-23	PROTACs Bcr-Abl	Cancer
ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells .

HY-161323

FLT3-ITD/D835Y-IN-1	FLT3 Bcr-Abl Apoptosis	Cancer
FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and *BCR-ABL* inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .

HY-15738

GNF-5 3 Publications Verification	Bcr-Abl	Cancer
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active *Bcr-Abl* inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC₅₀ value of 0.22 μM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer .

HY-15728

Radotinib IY-5511	Bcr-Abl	Cancer
Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.

HY-117718

AG957 Tyrphostin AG957; NSC 654705	Bcr-Abl	Cancer
AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity . AG957 is a *bcr/abl* kinase inhibitor with an IC₅₀ of 2.9 μM for p210 ^bcr/abl autokinase activity .

HY-101489A

GZD856 formic	PDGFR Bcr-Abl Apoptosis	Cancer
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC₅₀s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl ^T315I inhibitor, with IC₅₀s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity . GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15814

HG-7-85-01	Bcr-Abl PDGFR c-Kit Src JAK Apoptosis	Cancer
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of *Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl* kinase, KDR and RET with IC₅₀s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC₅₀>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis**, and inhibition of cell-cycle progression .

HY-10181

Dasatinib Maximum Cited Publications 99 Publications Verification BMS-354825	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.

HY-10181A

Dasatinib hydrochloride Maximum Cited Publications 99 Publications Verification BMS-354825 hydrochloride	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.

HY-10181B

Dasatinib monohydrate Maximum Cited Publications 99 Publications Verification BMS-354825 monohydrate	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.

HY-120036

Tyrphostin AG1112	Casein Kinase Tyrosinase	Cancer
Tyrphostin AG1112 is a potent inhibitors of CK II. Tyrphostin AG1112 inhibits p210 ^bcr-abl tyrosine kinase, with IC₅₀ values of 2, 15, 20 μM in p210 ^bcr-abl, EGFR and PDGFR cells, respectively .

HY-160478

GNF-6	Bcr-Abl	Cancer
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of *BCR-ABL-T315I* with IC₅₀s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .

HY-11007

GNF-2 2 Publications Verification	Bcr-Abl SARS-CoV	Cancer
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of *Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀* of 138 nM .

HY-128756

SIAIS178	PROTACs Bcr-Abl	Cancer
SIAIS178 is a potent and selective *BCR-ABL* degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity .

HY-10943

GNF-7 2 Publications Verification	Bcr-Abl Ack1	Cancer
GNF-7 is a multikinase inhibitor. GNF-7 is a *Bcr-Abl* inhibitor, with IC₅₀s of 133 nM and 61 nM for Bcr-Abl ^WT and Bcr-Abl ^T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC₅₀s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies .

HY-10181R

Dasatinib (Standard)	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits *Bcr-Abl* and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.

HY-137460

Vodobatinib K0706	Bcr-Abl	Cancer
Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC₅₀ of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research . Vodobatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-125834

GMB-475	PROTACs Bcr-Abl Apoptosis STAT JAK	Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .

HY-10181S

Dasatinib-d8 BMS-354825-d₈	Bcr-Abl Src Apoptosis Autophagy	Cancer
Dasatinib-d₈ is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

HY-108704

CT-721	Bcr-Abl	Cancer
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC₅₀ of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities . CT-721 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-13905

Flumatinib mesylate 1 Publications Verification HHGV678 mesylate	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of *Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀* values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .

Cat. No.	Product Name

HY-L196

Protein Kinase Compound Library

2,807 compounds

Protein Kinases (PTKs) are a class of phosphotransferases that phosphorylate proteins. Protein kinases participate in many signal transduction pathways including those involved with growth, differentiation, and cell division. Protein kinase not only plays an important role in the process of cell activation, but also its abnormal expression is closely related to the pathogenesis of many diseases. So far, the protein kinase family has become one of the most important drug targets. The most common drug targets include ALK, B-Raf, BCR-Abl, EGFR, and VEGFR.

MCE designs a unique collection of 2,807 bioactive compounds targeting protein kinases, which is an important tool for the development of drug targeting protein kinases.

HY-L129

Target Protein Ligand Library

37 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 37 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

HY-L080

Targeted Therapy Drug Library

107 compounds

Targeted cancer therapies are drugs or other substances that block the growth and spread of cancer by interfering with specific molecular targets that are involved in the growth, progression, and spread of cancer.

There are several different types of targeted therapy. The most common types are small-molecule drugs and monoclonal antibodies. Small-molecule drugs are small enough to enter cells easily, so they are used for targets that are inside cells, while monoclonal antibodies are usually used for targets that are located outside the cells. Because of high specificity, low side effect and potent anticancer activity, targeted therapy has become the mainstream of new anti-tumor drugs. Various targeted therapies have been approved by FDA and used in the treatment of diseases.

MCE carefully collects a unique of 107 targeted therapy drugs used in cancer treatment. MCE Targeted therapy drug library is a useful tool for the research of targeted therapy.

HY-L016

Protein Tyrosine Kinase Compound Library

1,064 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,064 compounds that act as a useful tool for PTKs-related drug screening and disease research.

HY-L060

Cytoskeleton Compound Library

1,328 compounds

The cytoskeleton is responsible for contraction, cell motility, movement of organelles and vesicles through the cytoplasm, cytokinesis, intracellular signal transduction, and many other functions that are essential for cellular homeostasis and survival. It accomplishes these tasks through three basic structures: F-actin, microtubules, and intermediate filaments (IFs). The cytoskeleton is a dynamic structure where the three major filaments and tubules are under the influence of proteins that regulate their length, state of polymerization, and level of cross-linking. Since cytoskeleton is involved in virtually all cellular processes, cytoskeletal protein aberrations are the underlying reason for many pathological phenotypes, including several cardiovascular disease syndromes, neurodegeneration, cancer, liver cirrhosis, pulmonary fibrosis, and blistering skin diseases.

MCE designs a unique collection of 1,328 cytoskeleton-related compounds mainly focusing on the key targets in the cytoskeleton signal pathway and can be used in the research of cytoskeleton signal pathway and related diseases.

HY-L079

Anti-Blood Cancer Compound Library

2,748 compounds

Blood cancers, also called hematologic cancers, occur when abnormal blood cells start growing out of control, interrupting the function of normal blood cells, which fight off infection and produce new blood cells. Most blood cancers start in the bone marrow, which is where blood is produced. There are three main types of blood cancers: leukemia, lymphoma and myeloma, which afflict millions of children and adults every year, and are often deadly.

Some common blood cancer treatments include stem cell transplantation, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. As we begin to understand the key signaling pathways and molecular drivers of malignant transformation in haematological disorders, new treatment strategies will continue to be developed.

MCE offers a unique collection of 2,748 compounds with identified and potential anti-blood cancer activity. These compounds target blood cancer’s major targets and signaling pathways. MCE anti-blood cancer compound library is a useful tool for anti-blood cancer drugs screening and other related research.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-108486

Herbimycin A	Infection Quinones Structural Classification Microorganisms Classification of Application Fields Source classification Benzene Quinones Disease Research Fields	Bacterial Antibiotic
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 ^v-src and p210 ^BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.

Cat. No.	Product Name	Chemical Structure

HY-10159S

Nilotinib-d6
Nilotinib-d₆ is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].

HY-10181S

Dasatinib-d8
Dasatinib-d₈ is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

HY-15463S

Imatinib-d8 1 Publications Verification
Imatinib-d₈ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-15463S1

Imatinib-d4
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-15463S2

Imatinib-d3 hydrochloride

Imatinib-d₃ (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

HY-132549S

Nilotinib-d3
Nilotinib-d₃ is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].

HY-10159S1

Nilotinib-13C,d3
Nilotinib-13C,d3 is a deuterated labeled Nilotinib . Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-13904S

Flumatinib-d3
Flumatinib-d₃ is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].

HY-133794S

Dasatinib N-oxide-d8
Dasatinib N-oxide-d₈ is the deuterium labeled Dasatinib N-oxide. Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].

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