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Results for "

AML MV4-11

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (6) AMPK (1) Apoptosis (31) ATF6 (1) ATM/ATR (1) Autophagy (1) Bcl-2 Family (6) Bcr-Abl (1) c-Myc (6) Casein Kinase (1) Caspase (5) CDK (10) Ceramidase (1) Checkpoint Kinase (Chk) (2) Deubiquitinase (1) DNA Methyltransferase (1) DNA/RNA Synthesis (2) Drug Derivative (1) DYRK (2) E3 Ligase Ligand-Linker Conjugates (2) Epigenetic Reader Domain (9) ERK (4) Fat Mass and Obesity-associated Protein (FTO) (2) FLT3 (26) HDAC (7) Histone Acetyltransferase (1) Histone Demethylase (3) Histone Methyltransferase (2) Interleukin Related (1) JAK (2) Ligands for Target Protein for PROTAC (2) Microtubule/Tubulin (1) Mitochondrial Metabolism (2) MNK (1) mTOR (2) p38 MAPK (2) p97 (1) PARP (4) Phosphatase (1) PI3K (2) Pim (1) Polo-like Kinase (PLK) (1) PROTAC-Linker Conjugates for PAC (1) PROTACs (11) RAR/RXR (1) Ras (1) Salt-inducible Kinase (SIK) (2) SHP2 (1) STAT (8) WDR5 (1) Wee1 (1)
By Research Areas:	Cancer (70) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (1)

By Targets:

Akt (6)

AMPK (1)

Apoptosis (31)

ATF6 (1)

ATM/ATR (1)

Autophagy (1)

Bcl-2 Family (6)

Bcr-Abl (1)

c-Myc (6)

Casein Kinase (1)

Caspase (5)

CDK (10)

Ceramidase (1)

Checkpoint Kinase (Chk) (2)

Deubiquitinase (1)

DNA Methyltransferase (1)

DNA/RNA Synthesis (2)

Drug Derivative (1)

DYRK (2)

E3 Ligase Ligand-Linker Conjugates (2)

Epigenetic Reader Domain (9)

ERK (4)

Fat Mass and Obesity-associated Protein (FTO) (2)

FLT3 (26)

HDAC (7)

Histone Acetyltransferase (1)

Histone Demethylase (3)

Histone Methyltransferase (2)

Interleukin Related (1)

JAK (2)

Ligands for Target Protein for PROTAC (2)

Microtubule/Tubulin (1)

Mitochondrial Metabolism (2)

MNK (1)

mTOR (2)

p38 MAPK (2)

p97 (1)

PARP (4)

Phosphatase (1)

PI3K (2)

Pim (1)

Polo-like Kinase (PLK) (1)

PROTAC-Linker Conjugates for PAC (1)

PROTACs (11)

RAR/RXR (1)

Ras (1)

Salt-inducible Kinase (SIK) (2)

SHP2 (1)

STAT (8)

WDR5 (1)

Wee1 (1)

By Research Areas:

Cancer (70)

Inflammation/Immunology (4)

Metabolic Disease (1)

Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-X0009

Tambiciclib 1 Publications Verification GFH009; JSH-009; SLS009	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Metabolic Disease Inflammation/Immunology Cancer
Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research .

HY-159657

PF-07899895	Salt-inducible Kinase (SIK) Interleukin Related	Inflammation/Immunology
PF-07899895 (Compound 34) is a SIK inhibitor, with IC₅₀ values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases .

HY-128724

CB-5339 2 Publications Verification	p97	Cancer
CB-5339 is an oral activity potent p97 inhibitor with an IC₅₀ <30 nM. CB-5339 can be used for leukemia research . CB-5339 extracted from WO2015109285A1 compound FF07.

HY-124500

AC-4-130 Maximum Cited Publications 6 Publications Verification	STAT Apoptosis	Cancer
AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .

HY-172581

Clifutinib	FLT3 Apoptosis Ras p38 MAPK PI3K Akt JAK STAT	Cancer
Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC₅₀ value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC₅₀ = 1.5 nM; MOLM-13: IC₅₀ = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia .

HY-161615

PROTAC ATR degrader-2	PROTACs ATM/ATR Apoptosis	Inflammation/Immunology Cancer
PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC₅₀ values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC₅₀ of 29.6 nM against ATR, and its IC₅₀ values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia .

HY-153886

Wu-5 1 Publications Verification	FLT3 AMPK Apoptosis Deubiquitinase	Cancer
Wu-5 is a USP10 inhibitor that can inhibit FLT3 and AMPK pathways, induce FLT3-ITD degradation and induce apoptosis .

HY-132182

HPA-12 1 Publications Verification	Ceramidase Autophagy Apoptosis ATF6	Neurological Disease Cancer
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .

HY-120084

BTX161 1 Publications Verification	Casein Kinase	Cancer
BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.

HY-114414

HDACs/mTOR Inhibitor 1 1 Publications Verification	HDAC mTOR Apoptosis	Cancer
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC₅₀s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .

HY-138632

PROTAC BRD4 Degrader linker conjugate	PROTACs Epigenetic Reader Domain PROTAC-Linker Conjugates for PAC	Cancer
PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC₅₀ values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)) .\n

HY-125236

ZEN-3694 BET-IN-19	Epigenetic Reader Domain	Cancer
ZEN-3694 (Compound 146) is a BET inhibitor. ZEN-3694 inhibits hlL-6 mRNA transcription (IC₅₀ ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC₅₀ ≤0.3 uM). ZEN-3694 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC₅₀ ≤0.3 uM) .

HY-164515

ONC213	Apoptosis Mitochondrial Metabolism Caspase PARP	Cancer
ONC213 is an orally active αKGDH inhibitor. ONC213 can suppress mitochondrial respiration and elevate α-ketoglutarate levels by inhibiting αKGDH activity. ONC213 can induce cells apoptosis by inducing mitochondrial stress response and inhibiting translation of MCL-1. ONC213 can be used for the research of cancer, such as acute myeloid leukemia research (AML) .

HY-122623A

DB818 dihydrochloride	Apoptosis	Cancer
DB818 dihydrochloride is the dihydrochloride salt form of DB818 (HY-122623). DB818 dihydrochloride is an inhibitor for Homeobox A9 (HOXA9). DB818 dihydrochloride reduces the formation of HOXA9-DNA complexes, inhibits the growth and induces apoptosis in AML cell lines OCI/AML3, MV4-11, and THP-1 .

HY-178858

PROTAC FLT3/CHK1 Degrader-1	PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt	Cancer
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .

HY-174911

FLT3-IN-33	FLT3 Apoptosis	Cancer
FLT3-IN-33 (Compound 7r) is a FLT3 inhibitor with an IC₅₀ of 7.82  nM. FLT3-IN-33 has superior anticancer activities against acute myeloid leukemia (AML) cells, such as MV4-11 and MOLM-13 cells. FLT3-IN-33 significantly induces cell apoptosis and inhibits phosphorylation of FLT3 pathways. FLT3-IN-33 can be used for AML and other cancers research .

HY-148521

PROTAC FLT3/CDK9 degrader-1	CDK FLT3 PROTACs Apoptosis	Cancer
PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML .

HY-158377

CDK8/19-IN-2	CDK STAT	Cancer
CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 8/19 (CDK8 and CDK19) inhibitor, with IC₅₀ values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research .

HY-179267

FTO-IN-16	Fat Mass and Obesity-associated Protein (FTO) c-Myc RAR/RXR Apoptosis	Cancer
FTO-IN-16 (Compound 8a-1), a FTO-IN-15 (HY-179266) prodrug, is a potent FTO inhibitor. FTO-IN-16 suppresses acute myeloid leukemia (AML) cell viability, increases m ⁶A levels, downregulates c-Myc and CEBPA, and upregulates ASB2 and RARA. FTO-IN-16 induces apoptosis. FTO-IN-16 demonstrates strong in vivo efficacy in AML mouse xenografts. FTO-IN-16 can be used for the research of AML .

HY-163678

Pomalidomide-CO-C7-NH-CO-C3-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-CO-C7-NH-CO-C3-COOH is a conjugate of a ligand for E3 ligase and a linker. Pomalidomide-CO-C7-NH-CO-C3-COOH can be used for synthesis of PROTAC degrader ARM165 (HY-163677) .

HY-143238

FY-56	Histone Demethylase	Cancer
FY-56 is a highly potent and selective LSD1/KDM1A inhibitor (IC₅₀=42 nM) and exhibits high selectivity over MAO-A/B. FY-56 induces differentiation of MOLM-13 and MV4-11 cell and has the potential for AML research .

HY-149474

HDAC-IN-63	FLT3 HDAC Apoptosis	Cancer
HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC₅₀: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC₅₀: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML) .

HY-179272

Wee1/HDAC-IN-1	Wee1 HDAC Apoptosis	Cancer
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC₅₀ of 1.2 nM for Wee1 and IC₅₀ values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC₅₀ of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .

HY-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1	PROTACs FLT3 JAK Epigenetic Reader Domain	Cancer
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC₅₀ values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC₅₀ = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .

HY-115906

K783-0308	FLT3 MNK Apoptosis	Cancer
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC₅₀ values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC₅₀=10.5 µM) and MV-4-11 (IC₅₀=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .

HY-155529

FD1024	Pim	Cancer
FD1024 is PIM inhibitor (IC₅₀s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .

HY-170558

FW-1	FLT3 Apoptosis	Cancer
FW-1 is a type I inhibitor for FLT3 with IC₅₀ of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13 .

HY-175473

HI042	FLT3 Apoptosis	Cancer
HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC₅₀ values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-\|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML) .

HY-150562

CDK9-IN-19	CDK	Cancer
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .

HY-138831

AES-350	HDAC Apoptosis	Cancer
AES-350 is a potent and orally active HDAC6 inhibitor with an IC₅₀ and a K_i of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research .

HY-172399

FTO-IN-14	Fat Mass and Obesity-associated Protein (FTO) Apoptosis	Cancer
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC₅₀ of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC₅₀ for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .

HY-173212

PLK1-IN-13	Polo-like Kinase (PLK) c-Myc Apoptosis	Cancer
PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC₅₀: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC₅₀: 12.72 nM) and PLK3 (IC₅₀: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML) .

HY-178996

FLT3-IN-36	FLT3 Apoptosis Akt ERK PI3K STAT Mitochondrial Metabolism	Cancer
FLT3-IN-36 is a potent FLT3 inhibitor. FLT3-IN-36 exhibits antitumor activity against FLT3-mutated acute myeloid leukemia (AML) cells. FLT3-IN-36 induces cell cycle arrest, reduces mitochondrial membrane potential, and induces apoptosis, downregulating FLT3 and downstream protein expression (including AKT, ERK, PI3K, and STAT5). FLT3-IN-36 can be used for AML research .

HY-143286

PF15	PROTACs FLT3	Cancer
PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC₅₀ of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .

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-163803

CM-444	HDAC DNA Methyltransferase	Cancer
CM-444 is inhibitor for HDAC (IC₅₀ is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC₅₀ is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .

HY-X0009A

Tambiciclib dimaleate 1 Publications Verification GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Cancer
Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research .

HY-155226

FLT3-IN-21	FLT3 Apoptosis	Cancer
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC₅₀: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC₅₀: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .

HY-173141

mTOR inhibitor-26	mTOR	Cancer
mTOR inhibitor-26 (Compound HPT-11) is an inhibitor of mTOR with an IC₅₀ of 0.7 nM. It effectively inhibits the proliferation of AML cell lines Molm-13 and MV-4-11. mTOR inhibitor-26 exhibits antitumor activity and favorable metabolic stability, making it a promising candidate for cancer research .

HY-162293

CDK8-IN-14	CDK	Cancer
CDK8-IN-14 (compound 12) inhibits CDK8 with an IC₅₀ value of 39.2 nM and has anti-AML cell proliferation activity (molm-13 GC50 = 0.02±0.01μM, MV4-11 GC50 = 0.03±0.01μM) .

HY-147716

CDK8-IN-6	CDK	Cancer
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an K_d of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC₅₀s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer .

HY-147717

CDK8-IN-7	CDK	Cancer
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an K_d of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC₅₀s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .

HY-178020

FLT3-IN-34	FLT3 ERK Akt Apoptosis	Cancer
FLT3-IN-34 is a FLT3 inhibitor, with an IC₅₀ value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC₅₀ = 14.95 nM) and MOLM-13 (IC₅₀ = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML) .

HY-170237

SIK2/3-IN-1	Salt-inducible Kinase (SIK)	Cancer
SIK2/3-IN-1 (Compound 7S) is a selectively inhibitory agent of SIK2/3 with oral activity. SIK2/3-IN-1 can significantly inhibit tumor growth (without any body weight loss) in the MV4-11 AML mice CDX model. SIK2/3-IN-1 can be used in the research of MEF2C-dependent acute myeloid leukemia .

HY-161710

XYD129	PROTACs Epigenetic Reader Domain Histone Acetyltransferase	Cancer
XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC ₅₀=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .

HY-174437A

FLT3-IN-32 TFA	FLT3	Cancer
FLT3-IN-32 TFA is a potent FLT3 inhibitor with an IC₅₀s of 2.40 nM and 3.83 nM against FLT3-ITD and FLT3-D835Y. FLT3-IN-32 TFA inhibits proliferation/survival of human MV4-11 cells with an IC₅₀ of 0.07 nM. FLT3-IN-32 TFA can be used for the study of acute myeloid leukemia (AML) .

HY-143895

FLT3-IN-12	FLT3	Cancer
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC₅₀ of 0.75 nM) .

HY-155112

Antiproliferative agent-30	Microtubule/Tubulin FLT3 Bcr-Abl	Cancer
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC₅₀s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .

HY-143894

FLT3-IN-11	FLT3	Cancer
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC₅₀ of 3.2 nM) .

HY-170576

FLT3-IN-28	FLT3 STAT Apoptosis	Cancer
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC₅₀ values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .

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AML MV4-11

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