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Results for "

Bcr-abl

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bcr-Abl (155) Ack1 (1) Akt (3) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (1) Apoptosis (46) ATTECs (1) Aurora Kinase (3) Autophagy (34) Bacterial (3) Bcl-2 Family (1) c-Kit (15) c-Myc (3) Casein Kinase (1) Caspase (3) CDK (2) Deubiquitinase (2) Drug Intermediate (1) Drug Metabolite (6) E3 Ligase Ligand-Linker Conjugates (2) EGFR (1) ERK (1) FLT3 (4) HDAC (3) Histone Methyltransferase (1) HSP (4) HyT (1) IGF-1R (3) Insulin Receptor (2) Isotope-Labeled Compounds (7) JAK (7) Ligands for E3 Ligase (3) Ligands for Target Protein for PROTAC (3) Microtubule/Tubulin (2) Mitosis (3) p38 MAPK (4) PARP (4) PDGFR (17) Prion Protein (3) PROTACs (18) Reference Standards (19) SARS-CoV (8) Small Interfering RNA (siRNA) (1) SNIPERs (12) Src (20) STAT (9) Target Protein Ligand-Linker Conjugates (2) Thymidylate Synthase (1) Tyrosinase (1) β-catenin (1)
By Research Areas:	Cancer (172) Cardiovascular Disease (2) Endocrinology (3) Infection (7) Inflammation/Immunology (8) Neurological Disease (9)
Oligonucleotides:	Human Pre-designed siRNA Sets (1) siRNAs (1)

180

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

GMP Molecules

Targets Recommended: Bcr-Abl

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10181

Dasatinib Maximum Cited Publications 168 Publications Verification BMS-354825	Bcr-Abl Src Autophagy Apoptosis Ligands for Target Protein for PROTAC	Infection Neurological Disease Inflammation/Immunology 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, and can cross the blood-brain barrier .

HY-10159

Nilotinib 45+ Cited Publications AMN107	Bcr-Abl Autophagy	Cancer
Nilotinib is an orally available *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity.

HY-50946

Imatinib Mesylate 115+ Cited Publications STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Infection Neurological Disease Inflammation/Immunology Cancer
Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, *Bcr-Abl, and PDGFR* (IC₅₀=100 nM) tyrosine kinases.

HY-104010

Asciminib 10+ Cited Publications abl001	Bcr-Abl	Cancer
Asciminib (ABL001) is a potent and selective allosteric *BCR-ABL1* inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM .

HY-15666

Olverembatinib 5+ Cited Publications 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-10181A

Dasatinib hydrochloride Maximum Cited Publications 168 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-10159A

Nilotinib monohydrochloride monohydrate 45+ 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-10181B

Dasatinib monohydrate Maximum Cited Publications 168 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-104010A

Asciminib hydrochloride 10+ Cited Publications abl001 hydrochloride	Bcr-Abl	Cancer
Asciminib (ABL001) hydrochloride is a potent and selective allosteric *BCR-ABL1* inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM .

HY-11007

GNF-2 3 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-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-137460

Vodobatinib 2 Publications Verification 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-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-15666A

Olverembatinib dimesylate 5+ Cited Publications 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-15738

GNF-5 4 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-13905

Flumatinib mesylate 3 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 .

HY-118144

PD166326	Src Bcr-Abl p38 MAPK	Cancer
PD166326 is an orally active tyrosine kinase inhibitor with a IC₅₀ of 8 nM against abl tyrosine kinase and a IC₅₀ of 6 nM against src tyrosine kinase. PD166326 blocks *Bcr/Abl* kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia .

HY-10181S

Dasatinib-d8 1 Publications Verification BMS-354825-d₈	Bcr-Abl Src Apoptosis Autophagy	Cancer
Dasatinib-d₈ (BMS-354825-d₈) is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

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-153996

CT1113	Deubiquitinase Apoptosis Bcr-Abl STAT c-Myc	Cancer
CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total *BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL*1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia .

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-103274

PD180970	Bcr-Abl Src c-Kit Apoptosis	Neurological Disease Cancer
PD180970 is a highly potent and ATP-competitive p210 ^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210 ^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .

HY-125845

(S,R,S)-AHPC 2 Publications Verification VH032-NH2; VHL ligand 1	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC₅₀ of 1.11 μM in Ba/F3 cells .

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-152036A

SIAIS100 TFA	PROTACs Bcr-Abl	Cancer
SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC₅₀ value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML) .

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 .

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-130297

*PROTAC BCR-ABL1 ligand 1*	Bcr-Abl Ligands for Target Protein for PROTAC	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-10159C

Nilotinib hydrochloride dihydrate 45+ Cited Publications AMN107 hydrochloride dihydrate	Autophagy Bcr-Abl	Cancer
Nilotinib (AMN107) hydrochloride dihydrate is an orally active *Bcr-Abl* tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia .

HY-145887

BCR-ABL1-IN-1	Bcr-Abl	Cancer
BCR-ABL1-IN-1 (Example 74) is the inhibitor for ABL1 (64-515) with IC₅₀ of 8.7 nM. BCR-ABL1-IN-1 can be used in research on diseases related to the central nervous system (CNS) .

HY-10181R

Dasatinib (Standard) BMS-354825 (Standard)	Reference Standards 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-10181S1

Dasatinib-d4 BMS-354825-d₄	Isotope-Labeled Compounds Autophagy Bcr-Abl Apoptosis Src	Cancer
Dasatinib-d₄ (BMS-354825-d₄) is deuterium labeled Dasatinib. 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-120508

Pivanex AN-9; Pivalyloxymethyl butyrate	HDAC Bcr-Abl Apoptosis	Inflammation/Immunology Cancer
Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates *bcr-abl* protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties .

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-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-10159R

Nilotinib (Standard) AMN107 (Standard)	Reference Standards 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 45+ Cited Publications 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-179247

BCR-ABL1-IN-2	Bcr-Abl	Cancer
BCR-ABL1-IN-2 (compound 8) is a potent BCR-ABL1 tyrosine kinase inhibitor. BCR-ABL1-IN-2 exhibits activity in Imatinib (HY-15463) resistant K562/DOX cells with LC₅₀ of 5.29 μM. BCR-ABL1-IN-2 shows no significant toxicity in nontumor cells. BCR-ABL1-IN-2 can be used for chronic myeloid leukemia research .

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-111872

SNIPER(ABL)-020	SNIPERs Bcr-Abl	Cancer
SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of *BCR-ABL* protein .

HY-150908

Brigatinib A	Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib A is an GID4 ligand. Brigatinib A can be used for synthesizing PROTAC BCR-ABL Degrader-2 (HY-174368) .

HY-152036

SIAIS100	PROTACs Bcr-Abl	Cancer
SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC₅₀ value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML) .

HY-111860

SNIPER(ABL)-013	SNIPERs Bcr-Abl	Cancer
SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of *BCR-ABL* protein with a DC₅₀ of 20 μM .

HY-111861

SNIPER(ABL)-024	SNIPERs Bcr-Abl	Cancer
SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of *BCR-ABL* protein with a DC₅₀ of 5μM .

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-10364

AP24163	Bcr-Abl	Cancer
AP24163 is a *BCR-ABL* kinase inhibitor. AP24163 inhibits wild-type (native) *BCR-ABL* and *BCR-ABL-T315I* with IC₅₀ values of 7 nM and 511 nM, respectively. AP24163 can be used in the research of chronic myeloid leukemia (CML) .

HY-180967

*PROTAC BCR-ABL* Degrader-2**	Bcr-Abl PROTACs Apoptosis	Cancer
PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl ^T315 PROTAC degrader with a DC₅₀ of 108.7 nM in Ba/F3 Bcr-Abl ^T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research .

Cat. No.	Product Name

HY-L196

Protein Kinase Compound Library

4,332 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 4,332 bioactive compounds targeting protein kinases, which is an important tool for the development of drug targeting protein kinases.

HY-L129

Target Protein Ligand Library

94 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 94 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

108 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 108 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

1,578 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 1,578 compounds that act as a useful tool for PTKs-related drug screening and disease research.

HY-L060

Cytoskeleton Compound Library

2,148 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 2,148 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

4,121 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 4,121 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	Type

HY-10181GL

Dasatinib (GMP Like)

BMS-354825 (GMP Like)

Fluorescent Dye

Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.

Cat. No.	Product Name	Type

HY-10181GL

Dasatinib (GMP Like)

BMS-354825 (GMP Like)

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Area

HY-P11435

KQSSKALQR	Peptides	Cancer
KQSSKALQR is a BCR-ABL peptide. KQSSKALQR can induce CD8 ⁺T cell responses. KQSSKALQR can be used in vaccine research for chronic myeloid leukaemia (CML) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-108486

Herbimycin A	Infection Quinones Microorganisms Classification of Application Fields Benzene Quinones Disease Research Fields Source Classification	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.

HY-125780R

5-Phenylhydantoin (Standard)	Microorganisms Source Classification	Drug Metabolite Reference Standards
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis 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.

Cat. No.	Product Name	Chemical Structure

HY-10181S

Dasatinib-d8 1 Publications Verification
Dasatinib-d₈ (BMS-354825-d₈) is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

HY-15463S1

Imatinib-d4
Imatinib-d₄ (STI571-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 .

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 .

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 .

HY-10159S

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

HY-10181S1

Dasatinib-d4

Dasatinib-d₄ (BMS-354825-d₄) is deuterium labeled Dasatinib. 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-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 .

HY-15463S3

Imatinib-13C,d3

Imatinib- ¹³C,d₃ (STI571- ¹³C,d₃) is ¹³C 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 .

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-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-15728S

Radotinib-d6

Radotinib-d₆ is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .

Targets Recommended: Bcr-Abl

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10181G

Dasatinib (GMP) BMS-354825 (GMP)	Src Bcr-Abl Apoptosis Autophagy	Cancer
Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual *Src/Bcr-Abl* inhibitor with potent antitumor activity. The K_i values for Src and *Bcr-Abl* are 16 pM and 30 pM, respectively. Dasatinib inhibits *Bcr-Abl* and Src with IC₅₀ values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy .

HY-10181GL

Dasatinib (GMP Like) BMS-354825 (GMP Like)	Bcr-Abl Src Autophagy Apoptosis	Cancer
Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.

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