Search Result

Results for "

Acute myeloid leukemia target

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Antibody (2) Apoptosis (11) Aurora Kinase (2) Bcr-Abl (1) Biochemical Assay Reagents (1) Btk (1) c-Kit (3) c-Myc (1) Casein Kinase (1) CD3 (2) CDK (1) DNA Methyltransferase (1) DNA/RNA Synthesis (1) Epigenetic Reader Domain (6) Ferroptosis (1) FLT3 (4) GSK-3 (1) HDAC (1) Histone Methyltransferase (1) HSP (1) Interleukin Related (1) Isocitrate Dehydrogenase (IDH) (1) MDM-2/p53 (1) Molecular Glues (4) Mps1 (2) PROTACs (10) Proteasome (1) Reactive Oxygen Species (ROS) (1) RET (1) Ribosomal S6 Kinase (RSK) (1) Small Interfering RNA (siRNA) (1) STAT (1) TET Protein (1) Transmembrane Glycoprotein (5) WDR5 (1) Wee1 (1)
By Research Areas:	Cancer (42) Infection (1) Inflammation/Immunology (4)

By Targets:

ADC Antibody (2)

Apoptosis (11)

Aurora Kinase (2)

Bcr-Abl (1)

Biochemical Assay Reagents (1)

Btk (1)

c-Kit (3)

c-Myc (1)

Casein Kinase (1)

CD3 (2)

CDK (1)

DNA Methyltransferase (1)

DNA/RNA Synthesis (1)

Epigenetic Reader Domain (6)

Ferroptosis (1)

FLT3 (4)

GSK-3 (1)

HDAC (1)

Histone Methyltransferase (1)

HSP (1)

Interleukin Related (1)

Isocitrate Dehydrogenase (IDH) (1)

MDM-2/p53 (1)

Molecular Glues (4)

Mps1 (2)

PROTACs (10)

Proteasome (1)

Reactive Oxygen Species (ROS) (1)

RET (1)

Ribosomal S6 Kinase (RSK) (1)

Small Interfering RNA (siRNA) (1)

STAT (1)

TET Protein (1)

Transmembrane Glycoprotein (5)

WDR5 (1)

Wee1 (1)

By Research Areas:

Cancer (42)

Infection (1)

Inflammation/Immunology (4)

Inhibitors & Agonists

Inhibitory Antibodies

Targets Recommended: TREM receptor Target Protein Ligand-Linker Conjugates BMI1 Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P99958

Vixtimotamab AMV-564; TandAb T564	Transmembrane Glycoprotein	Cancer
Vixtimotamab (AMV-564; TandAb T564) is a bispecific tetravalent tandem diabody (TandAb) that targets human CD33 and human CD3 antigens. Vixtimotamab can be used for the research of acute myeloid leukemia (AML) .

HY-P99971

Gemtuzumab	ADC Antibody Transmembrane Glycoprotein	Cancer
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen. Gemtuzumab affects cell necrosis by specifically targeting CD33 expressed on the surface of leukaemic cell blasts in acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .

HY-120035

DD1	Proteasome Ribosomal S6 Kinase (RSK) Apoptosis	Cancer
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation .

HY-120395

UC-514321 1 Publications Verification	STAT Apoptosis TET Protein	Inflammation/Immunology Cancer
UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity .

HY-168475

DD0-2363	Apoptosis WDR5 HDAC	Cancer
DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .

HY-P991558

RO-5429083 RG-7356	Transmembrane Glycoprotein	Cancer
RO-5429083 is a humanized monoclonal antibody inhibitor targeting CD44. RO-5429083 can be used for acute myeloid leukemia (AML) and solid tumors research .

HY-114162B

VTP50469 mesylate	Epigenetic Reader Domain Apoptosis	Cancer
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.

HY-124629A

DB2313 tetrahydrochloride	Apoptosis	Cancer
DB2313 tetrahydrochloride is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 tetrahydrochloride disrupts the interaction of PU.1 with target gene promoters. DB2313 tetrahydrochloride induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects .

HY-P991425

AT-1413	Transmembrane Glycoprotein	Cancer
AT-1413 is a human monoclonal antibody (mAb) targeting CD43. AT-1413 induces antibody-dependent cell-mediated cytotoxicity (ADCC) in melanoma cell lines and acute myeloid leukemia (AML) cells. AT-1413 has antitumor activity in AML mouse models. AT-1413 can be used in Acute myeloid leukaemia, Breast cancer, Malignant melanoma and Myelodysplastic syndromes research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .

HY-171792

BMS-986497 ORM-6151	Transmembrane Glycoprotein	Cancer
BMS-986497 (ORM-6151) is a *CD33*-targeted antibody-conjugated GSPT1 degrader. BMS-986497 delivers the GSPT1 degrader SMol006 to CD33-expressing cells, inducing GSPT1 protein degradation. BMS-986497 is promising for research of acute myeloid leukemia (AML) .

HY-30272

Monobenzone 1 Publications Verification	Biochemical Assay Reagents Apoptosis DNA/RNA Synthesis	Cancer
Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and Apoptosis .

HY-107458

AP23848	c-Kit	Cancer
AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .

HY-157334

DEG-77	Molecular Glues Casein Kinase	Cancer
DEG-77, is a IKZF2 and CK1α targeted molecular glue, with DC₅₀s of 15.3 nM and 10 nM, respectively. DEG-77 possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t_1/2=8h). DEG-77 can be used for acute myeloid leukemia (AML) study .

HY-124629

DB2313 3 Publications Verification	Apoptosis	Cancer
DB2313 is a potent inhibitor of transcription factor PU.1. DB2313 inhibits PU.1-dependent reporter gene transactivation with an IC₅₀ of 5 μM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis in acute myeloid leukemia (AML) cells and has anticancer effects .

HY-115881

SR-1114	PROTACs Epigenetic Reader Domain	Cancer
SR-1114 is a PROTAC degrader targeting ENL. SR-1114 degrades ENL in a CRBN-dependent manner and selectively downregulates ENL target genes. SR-1114 can promote the differentiation of acute myeloid leukemia cells. SR-1114 can be used in tumor research. (Pink: ENL ligand (HY-145409); Black: Linker; Blue: E3 Ligand (HY-14658)) .

HY-169937

(R)-SR-C-107	Epigenetic Reader Domain	Cancer
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC₅₀ and K_D of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .

HY-108894

Ferumoxytol	Reactive Oxygen Species (ROS) Ferroptosis	Cancer
Ferumoxytol is an iron oxide nanoparticle. Ferumoxytol has anti-leukemic activity, especially against acute myeloid leukemia (AML) cells with low iron transporter protein (FPN) expression. Ferumoxytol increases intracellular iron content, triggers the Fenton reaction, generates reactive oxygen species (ROS), leads to oxidative stress and ferroptosis. Ferumoxytol can selectively kill leukemic cells with low FPN expression while avoiding toxicity to normal cells. Ferumoxytol can be used to study leukemias with targeted iron metabolism abnormalities .

HY-P99623

Flotetuzumab MGD006; S80880	CD3	Cancer
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .

HY-176732

MJ-26	Epigenetic Reader Domain	Cancer
MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (K_i: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research .

HY-173274

CB039	Molecular Glues	Cancer
CB039 is a selective a molecular glue degrader that targets RBM39 (RNA-binding protein 39). CB039 promotes the formation of a ternary complex between RBM39 and the E3 ubiquitin ligase CUL4-DCAF15, leading to proteasomal degradation of RBM39. CB039 is promising for research of cancers with RBM39 dependency, such as acute myeloid leukemia (AML) and ovarian cancer .

HY-163707

UR778Br	Apoptosis	Cancer
UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .

HY-149539

PLM-101	FLT3 RET	Cancer
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .

HY-173631

(S)-dHTC1	PROTACs	Cancer
(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC₅₀ value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC₅₀ value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study .

HY-157213

LWY713	Apoptosis PROTACs FLT3	Cancer
LWY713 is a PROTAC-class FLT3 degrader (DC₅₀=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).

HY-168540

PROTAC MPS1 degrader 1	PROTACs Mps1 Aurora Kinase	Cancer
PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC₅₀s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984) .

HY-168543

PROTAC MPS1 degrader 2	PROTACs Aurora Kinase Mps1	Cancer
PROTAC MPS1 degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1，TTK)，AURKA and AURKB，with DC₅₀s of 42.0，2.1 and 154.0 nM，respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168545); Black: linker (HY-N0420); Blue: ligand for E3 ligase (HY-10984) .

HY-P99521

Vibecotamab XmAb14045	CD3	Inflammation/Immunology Cancer
Vibecotamab (XmAb14045) is a potent bispecific antibody targeting both CD123 and CD3. Vibecotamab targets T cell-mediated killing of CD123-expressing cells, regardless of T cell antigen specificity. Vibecotamab is a full length immunoglobulin molecule. Vibecotamab can be studied in research for diseases such as Myelodysplastic syndrome and acute myeloid leukemia. Recommend Isotype Control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .

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-176457

ZS3-046	Small Interfering RNA (siRNA) MDM-2/p53 PROTACs	Cancer
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176470)) .

HY-P991294

MGTA-117 Antibody	ADC Antibody	Cancer
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .

HY-144433

DNMT3A-IN-1 1 Publications Verification	DNA Methyltransferase	Infection
DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with K_I values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .

HY-134557

GS87	GSK-3	Cancer
GS87 is a highly specific and potent GSK3 inhibitor with IC₅₀s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research .

HY-145898

WBC100 14-D-Valine-TPL	c-Myc Molecular Glues	Cancer
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .

HY-164542

TQ05310	Isocitrate Dehydrogenase (IDH)	Cancer
TQ05310 is an orally available inhibitor of IDH2 mutants, targeting both IDH2-R140Q (IC₅₀=136.9 nM) and IDH2-R172K (IC₅₀=37.9 nM) mutants. TQ05310 inhibits the production of 2-hydroxyglutarate (2-HG) and induces differentiation of cells expressing IDH2-R140Q and IDH2-R172K by inhibiting the enzymatic activity of mutant IDH2. TQ05310 can be used for the study of acute myeloid leukemia .

HY-173333

PROTAC SMARCA2/4 degrader-38	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC₅₀: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)) .

HY-P99488

Briquilimab JSP-191; AMG-191	c-Kit	Inflammation/Immunology Cancer
Briquilimab (JSP-191 or AMG-191) is a humanized IgG1 monoclonal antibody that binds human CD117 (c-Kit). Briquilimab blocks the interaction between CD117 receptor and stem cell factor on various CD117 expressing tissues. Briquilimab can lead to inhibition of SCF/c-Kit signaling and MC apoptosis. Briquilimab is a non-toxic approach to target and deplete HSC, enabling blood and immune reconstitution with minimal toxicity with the other agents being used for transient immune suppression to prevent immunologic rejection. Briquilimab can be used in various disease research such as severe combined immunodeficiency (SCID), myelodyplastic syndromes (MDS), acute myeloid leukemia (AML), chronic spontaneous urticarial (CSU), chronic inducible urticarial (CIndU) and asthema .

HY-173320

HEMTAC WEE1 degrader-1	Wee1 HSP	Cancer
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC₅₀: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .

HY-P99395

Talacotuzumab 1 Publications Verification JNJ 56022473; CSL 362	Interleukin Related	Cancer
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has K_Ds of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .

HY-150797

QA-68 QA-68-ZU81	PROTACs Epigenetic Reader Domain	Inflammation/Immunology Cancer
QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).

HY-161708

PROTAC FLT3/CDKs degrader-1	PROTACs CDK FLT3	Cancer
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC₅₀ is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC₅₀s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))

HY-117947

(R)-OR-S1	Histone Methyltransferase	Cancer
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.

HY-153803

GBD-9	PROTACs Molecular Glues Btk	Cancer
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) . GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).

HY-121708

KI-328	c-Kit	Cancer
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.

Cat. No.	Product Name	Target	Research Area